Skip to main content
SpringerLink
Log in

α1-Adrenoceptors in the Urinary Tract

  • Chapter
  • First Online:
Urinary Tract

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 2011))

Abstract

α1-Adrenoceptors have been identified and characterized extensively by functional, radioligand-binding, and molecular biological techniques. Molecular clones have been isolated for three α1-subtypes (α1a, α1b, and α1d), and these subtypes are also functionally characterized. α1-Adrenoceptors are present in the prostate, urethra, bladder (urothelium, smooth muscle, and afferent nerves), ureter, vas deferens, peripheral ganglia, nerve terminals, vascular tissues, and central nervous system (CNS), and they could all potentially influence overall urinary function and contribute to both the therapeutic and adverse effects of α1-adrenoceptor antagonists in patients with benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS). This review aimed to discuss the relevant physiological and pharmacological roles and molecular biology of α1-adrenoceptor subtypes in the prostate, urethra, bladder, ureter, and CNS.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Log in via an institution
Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 259.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 329.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 329.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

References

  • Abrams P, Tammela TL, Hellström P, Marberger M, Djavan BR, Lunglmayr G, Panos P, Labal KU (1998) European pressure-flow investigation of tamsulosin in men with lower urinary tract symptoms (LUTS) suggestive of benign prostatic obstruction (BPO) – ESPRIT study. J Urol 159:256

    Google Scholar 

  • Akiyama K, Hora M, Tatemichi S, Masuda N, Nakamura S, Yamagishi R, Kitazawa M (1999) KMD-3213, a uroselective and long-acting α1a-adrenoceptor antagonist, tested in a novel rat model. J Pharmacol Exp Ther 291:81–91

    CAS  PubMed  Google Scholar 

  • Andersson KE (2002) Alpha-adrenoceptors and benign prostatic hyperplasia: basic principles for treatment with alpha-adrenoceptor antagonists. World J Urol 19:390–396

    CAS  PubMed  Google Scholar 

  • Andersson KE, Gratzke C (2007) Pharmacology of α1-adrenoceptor antagonists in the lower urinary tract and central nervous system. Nat Clin Pract Urol 4:368–378

    CAS  PubMed  Google Scholar 

  • Andersson KE, Larsson B, Sjogren C (1984) Characterization of the α-adrenoceptors in the female rabbit urethra. Br J Pharmacol 81:293–300

    CAS  PubMed  Google Scholar 

  • Beach MA, Mauro LS (2006) Pharmacologic expulsive treatment of ureteral calculi. Ann Pharmacother 40:1361–1368

    CAS  PubMed  Google Scholar 

  • Birder LA, de Groat WC (2007) Mechanisms of disease: involvement of the urothelium in bladder dysfunction. Nat Clin Pract Urol 4:46–54

    CAS  PubMed  Google Scholar 

  • Boyle P, Napalkov P (1995) The epidemiology of benign prostatic hyperplasia and observations on concomitant hypertension. Scand J Urol Nephrol Suppl 168:7–12

    CAS  PubMed  Google Scholar 

  • Bylund DB, Eikenberg DC, Hieble JP, Langer SZ, Lefkowitz RJ, Minneman KP, Molinoff PB, Ruffolo RR Jr, Trendelenburg U (1994) International Union of Pharmacology nomenclature of adrenoceptors. Pharmacol Rev 46:121–136

    CAS  PubMed  Google Scholar 

  • Caine M, Raz S, Zeigler M (1975) Adrenergic and cholinergic receptors in the human prostate, prostatic capsule and bladder neck. Br J Urol 47:193–202

    CAS  PubMed  Google Scholar 

  • Chang RS, Chen TB, O’Malley SS, Pettibone DJ, DiSalvo J, Francis B, Bock MG, Freidinger R, Nagarathnam D, Miao SW, Shen Q, Lagu B, Murali Dhar TG, Tyagarajan S, Marzabadi MR, Wong WC, Gluchowski C, Forray C (2000) In vitro studies on L-771, 688 (SNAP 6383), a new potent and selective α1a-adrenoceptor antagonist. Eur J Pharmacol 409:301–312

    CAS  PubMed  Google Scholar 

  • Chapple CR, Aubry ML, James S, Greengrass PM, Burnstock G, Turner-Warwick RT, Milroy EJ, Davey MJ (1989) Characterization of human prostatic adrenoceptors using pharmacology receptor binding and localization. Br J Urol 63:487–496

    CAS  PubMed  Google Scholar 

  • Chen Q, Takahashi S, Zhong S, Hosoda C, Zheng HY, Ogushi T, Fujimura T, Ohta N, Tanoue A, Tsujimoto G, Kitamura T (2005) Function of the lower urinary tract in mice lacking α1d-adrenoceptor. J Urol 174:370–374

    CAS  PubMed  Google Scholar 

  • Chueh SC, Guh JH, Chen J, Lai MK, Ko FN, Teng CM (1996) Inhibition by tamsulosin of tension responses of human hyperplastic prostate to electrical field stimulation. Eur J Pharmacol 305:177–180

    CAS  PubMed  Google Scholar 

  • Danuser H, Thor KB (1995) Inhibition of central sympathetic and somatic outflow to the lower urinary tract of the cat by the α1 adrenergic receptor antagonist prazosin. J Urol 153:1308–1312

    CAS  PubMed  Google Scholar 

  • Day HE, Campeau S, Watson SJ Jr, Akil H (1997) Distribution of α1a-, α1b- and α1d-adrenergic receptor mRNA in the rat brain and spinal cord. J Chem Neuroanat 13:115–139

    CAS  PubMed  Google Scholar 

  • de Groat WC, Booth AM, Yoshimura N (1993) Neurophysiology of micturition and its modification in animal models of human disease. In: Maggi CA (ed) The autonomic nervous system nervous control of the urogenital system, vol 6. Harwood Academic Publishers, London, p 227

    Google Scholar 

  • de Mey C, Michel MC, McEwen J, Moreland T (1998) A double-blind comparison of terazosin and tamsulosin on their differential effects on ambulatory blood pressure and nocturnal orthostatic stress testing. Eur Urol 33:481–488

    PubMed  Google Scholar 

  • Delaflotte S, Auguet M, Chabrier PE (1996) Pharmacological evidence that different α1 adrenoceptor subtypes mediate contraction in rabbit prostate and hypogastric artery. Acta Physiol Scand 158:241–251

    CAS  PubMed  Google Scholar 

  • Deng XF, Chemtob S, Varma DR (1996) Characterization of α1d- adrenoceptor subtype in rat myocardium, aorta and other tissues. Br J Pharmacol 119:269–276

    CAS  PubMed  Google Scholar 

  • Deplanne V, Palea S, Angel I (1998) The adrenergic, cholinergic and NANC nerve-mediated contractions of the female rabbit bladder neck and proximal, medial and distal urethra. Br J Pharmacol 123:1517–1524

    CAS  PubMed  Google Scholar 

  • Domyancic AV, Morilak DA (1997) Distribution of α1A adrenergic receptor mRNA in the rat brain visualized by in situ hybridization. J Comp Neurol 386:358–378

    CAS  PubMed  Google Scholar 

  • Eltze M, Boer R, Michel MC, Hein P, Testa R, Ulrich WR, Kolassa N, Sanders KH (2001) In vitro and in vivo uroselectivity of B8805-033, an antagonist with high affinity at prostatic α1A- vs. α1B- and α1D-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol 363:649–662

    CAS  PubMed  Google Scholar 

  • Fine SR, Ginsberg P (2008) Alpha-adrenergic receptor antagonists in older patients with benign prostatic hyperplasia: issues and potential complications. J Am Osteopath Assoc 108:333–337

    PubMed  Google Scholar 

  • Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA, Gluchowski C (1994) The α1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human α1c subtype. Mol Pharmacol 45:703–708

    CAS  PubMed  Google Scholar 

  • Fulton B, Wagstaff AJ, Sorkin EM (1995) Doxazosin. An update of its clinical pharmacology and therapeutic applications in hypertension and benign prostatic hyperplasia. Drugs 49:295–320

    CAS  PubMed  Google Scholar 

  • Guh JH, Chueh SC, Ko FN, Teng CM (1995) Characterization of α1-adrenoceptor subtypes in tension response of human prostate to electrical field stimulation. Br J Pharmacol 115:142–146

    CAS  PubMed  Google Scholar 

  • Guilmard C, Auguet M, Chabrier PE (1996) Pharmacological characterization of alpha1-adrenoceptor subtype mediating regulation of arterial pressure and urethral perfusion pressure in the anaesthetized rat. J Auton Pharmacol 16:197–203

    CAS  PubMed  Google Scholar 

  • Guimaraes S, Moura D (2001) Vascular adrenoceptors: an update. Pharmacol Rev 53:319–356

    CAS  PubMed  Google Scholar 

  • Hampel C, Dolber PC, Smith MP, Savic SL, JW Throff, Thor KB, Schwinn DA (2002) Modulation of bladder α1-adrenergic receptor subtype expression by bladder outlet obstruction. J Urol 167:1513–1521

    CAS  PubMed  Google Scholar 

  • Harada K, Ohmori M, Kitoh Y, Sugimoto K, Fujimura A (1999) A comparison of the antagonistic activities of tamsulosin and terazosin against human vascular α1-adrenoceptors. Jpn J Pharmacol 80:209–215

    CAS  PubMed  Google Scholar 

  • Hatano A, Takahashi H, Tamaki M, Komeyama T, Koizumi T, Takeda M (1994) Pharmacological evidence of distinct α1-adrenoceptor subtypes mediating the contraction of human prostatic urethra and peripheral artery. Br J Pharmacol 113:723–728

    CAS  PubMed  Google Scholar 

  • Hawrylyshyn KA, Michelotti GA, Coge F, Guenin SP, Schwinn DA (2004) Update on human α1-adrenoceptor subtype signaling and genomic organization. Trends Pharmacol Sci 25:449–455

    CAS  PubMed  Google Scholar 

  • Hiraoka Y, Ohmura T, Sakamoto S, Hayashi H, Muramatsu I (1995) Identification of α1-adrenoceptor subtypes in the rabbit prostate. J Auton Pharmacol 15:271–278

    CAS  PubMed  Google Scholar 

  • Hirasawa A, Horie K, Tanaka T, Takagaki K, Murai M, Yano J, Tsujimoto G (1993) Cloning, functional expression and tissue distribution of human cDNA for the α1C- adrenergic receptor. Biochem Biophys Res Commun 195:902–909

    CAS  PubMed  Google Scholar 

  • Hollingsworth JM, Rogers MA, Kaufman SR, Bradford TJ, Saint S, Wei JT, Hollenbeck BK (2006) Medical therapy to facilitate urinary stone passage: a meta-analysis. Lancet 368:1171–1179

    PubMed  Google Scholar 

  • Honda K, Miyata-Osawa A, Takenaka T (1985) α1-Adrenoceptor subtype mediating contraction of the smooth muscle in the lower urinary tract and prostate of rabbits. Naunyn Schmiedebergs Arch Pharmacol 330:16–21

    CAS  PubMed  Google Scholar 

  • Ishihama H, Momota Y, Yanase H, Wang X, de Groat WC, Kawatani M (2006) Activation of α1D adrenergic receptors in the rat urothelium facilitates the micturition reflex. J Urol 175:358–364

    CAS  PubMed  Google Scholar 

  • Ishizuka O, Persson K, Mattiasson A, Naylor A, Wyllie M, Andersson KE (1996) Micturition in conscious rats with and without bladder outlet obstruction: role of spinal α1-drenoceptors. Br J Pharmacol 117:962–966

    CAS  PubMed  Google Scholar 

  • Ishizuka O, Pandita RK, Mattiasson A, Steers WD, Andersson KE (1997) Stimulation of bladder activity by volume, l-dopa and capsaicin in normal conscious rats -effects of spinal α1-adrenoceptor blockade. Naunyn Schmiedebergs Arch Pharmacol 355:787–793

    CAS  PubMed  Google Scholar 

  • Itoh Y, Kojima Y, Yasui T, Tozawa K, Sasaki S, Kohri K (2007) Examination of alpha 1 adrenoceptor subtypes in the human ureter. Int J Urol 14:749–753

    CAS  PubMed  Google Scholar 

  • Jensen BC, Swigart PM, Simpson PC (2009) Ten commercial antibodies for alpha-1-adrenergic receptor subtypes are nonspecific. Naunyn-Schmiedebergs Arch Pharmacol 379:409–412

    CAS  PubMed  Google Scholar 

  • Jeong MS, Lee JG (2000) The role of spinal and peripheral α1- and α2- adrenoceptors on bladder activity induced by bladder distension in anaesthetized rat. BJU Int 85:925–931

    CAS  PubMed  Google Scholar 

  • Kawabe K (1998) Current status of research on prostate-selective alpha 1-antagonists. Br J Urol 81(Suppl 1):48–50

    CAS  PubMed  Google Scholar 

  • Kawabe K, Moriyama N, Hamada K, Ishima T (1990) Density and localization of alpha1-adrenoceptors in hypertrophied prostate. J Urol 143:592–595

    CAS  PubMed  Google Scholar 

  • Kawabe K, Moriyama N, Yamada S, Taniguchi N (1994) Rationale for the use of α-blockers in the treatment of benign prostatic hyperplasia (BPH). Int J Urol 1:203–211

    CAS  PubMed  Google Scholar 

  • Keast JR, Kawatani M, De Groat WC (1990) Sympathetic modulation of cholinergic transmission in cat vesical ganglia is mediated by α1- and α2-adrenoceptors. Am J Physiol 258:R44–50

    CAS  PubMed  Google Scholar 

  • Kenny BA, Naylor AM, Carter AJ, Read AM, Greengrass PM, Wyllie MG (1994) Effect of alpha1 adrenoceptor antagonists on prostatic pressure and blood pressure in the anesthetized dog. Urology 44:52–57

    CAS  PubMed  Google Scholar 

  • Kenny BA, Miller AM, Williamson IJ, O’Connell J, Chalmers DH, Naylor AM (1996) Evaluation of the pharmacological selectivity profile of α1- adrenoceptor antagonists at prostatic α1- adrenoceptors: binding, functional and in vivo studies. Br J Pharmacol 118:871–878

    CAS  PubMed  Google Scholar 

  • Killam AL, Watts SW, Cohen ML (1995) Role of α1- adrenoceptors and 5-HT2 receptors in serotonin-induced contraction of rat prostate: autoradiographical and functional studies. Eur J Pharmacol 273:7–14

    CAS  PubMed  Google Scholar 

  • Kobayashi S, Tang R, Shapiro E, Lepor H (1993) Characterization and localization of prostatic alpha 1 adrenoceptors using radioligand receptor binding on slide-mounted tissue section. J Urol 150:2002–2006

    CAS  PubMed  Google Scholar 

  • Kobayashi S, Tomiyama Y, Hoyano Y, Yamazaki Y, Hiroshi KUsama, Itoh Y, Kubota Y, Kohri K (2009a) Gene expressions and mechanical functions of α1-adrenoceptor subtypes in mouse ureter. World J Urol. doi:10.1007/s00345-009-0396-y

    PubMed  Google Scholar 

  • Kobayashi S, Tomiyama Y, Hoyano Y, Yamazaki Y, Kusama H, Kubota Y, Sasaki S, Kohri K (2009b) Mechanical function and gene expression of α1-adrenoceptor subtypes in dog intravesical ureter. Urology 74:458–462

    PubMed  Google Scholar 

  • Kunisawa Y, Kawabe K, Niijima T, Honda K, Takenaka T (1985) A pharmacological study of alpha adrenergic receptor subtypes in smooth muscle of human urinary bladder base and prostatic urethra. J Urol 134:396–398

    CAS  PubMed  Google Scholar 

  • Küpeli B, Irkilata L, Gürocak S, Tunç L, Kiraç M, Karaoğlan U, Bozkirli I (2004) Does tamsulosin enhance lower ureteral stone clearance with or without shock wave lithotripsy? Urology 64:1111–1115

    PubMed  Google Scholar 

  • Lagu B, Tian D, Jeon Y, Li C, Wetzel JM, Nagarathnam D, Shen Q, Forray C, Chang RS, Broten TP, Ransom RW, Chan TB, O’Malley SS, Schorn TW, Rodrigues AD, Kassahun K, Pettibone DJ, Freidinger RO, Gluchowski C (2000) De novo design of a novel oxazolidinone analogue as a potent and selective α1A adrenergic receptor antagonist with high oral bioavailability. J Med Chem 43:2775–2778

    CAS  PubMed  Google Scholar 

  • Larsson B, Sjogren C, Andersson KE (1986) Regional distribution of α-adrenoceptor subtypes in the female rabbit urethra. Acta Physiol Scand 126:39–43

    CAS  PubMed  Google Scholar 

  • Lefevre-Borg F, O’Connor SE, Schoemaker H, Hicks PE, Lechaire J, Gautier E, Pierre F, Pimoule C, Manoury P, Langer SZ (1993) Alfuzosin, a selective α1-adrenoceptor antagonist in the lower urinary tract. Br J Pharmacol 109:1282–1289

    CAS  PubMed  Google Scholar 

  • Lepor H (1998) Phase III multicenter placebo-controlled study of tamsulosin in benign prostatic hyperplasia. Tamsulosin Investigator Group. Urology 51:892–900

    CAS  PubMed  Google Scholar 

  • Lepor H, Lowe FC (2002) Evaluation and nonsurgical management of benign prostatic hyperplasia. In: Walch PC, Tetik AB, Vaughan ED (eds) Campbell’s urology, 8th edn. WB Saunders CO, Philadelphia, pp 1337–1378

    Google Scholar 

  • Lepor H, Zhang W, Kobayashi S, Tang R, Wang B, Shapiro E (1994) A comparison of the binding and functional properties of Alpha-1 adrenoceptors and area density of smooth muscle in the human, canine and rat prostates. J Pharmacol Exp Ther 270:722–727

    CAS  PubMed  Google Scholar 

  • Levin RM, Ruggieri MR, Wein AJ (1988) Identification of receptor subtypes in the rabbit and human urinary bladder by selective radio-ligand binding. J Urol 139:844–848

    CAS  PubMed  Google Scholar 

  • Lluel P, Deplanne V, Heudes D, Bruneval P, Palea S (2003) Age-related changes in urethrovesical coordination in male rats: relationship with bladder instability? Am J Physiol Regul Integr Comp Physiol 284:R1287–1295

    CAS  PubMed  Google Scholar 

  • Malloy BJ, Price DT, Price RR, Bienstock AM, Dole MK, Funk BL, Rudner XL, Richardson CD, Donatucci CF, Schwinn DA (1998) α1-adrenergic receptor subtypes in human detrusor. J Urol 160:937–943

    CAS  PubMed  Google Scholar 

  • Marks LS, Gittelman MC, Hill LA, Volinn W, Hoel G (2009) Silodosin in the treatment of the signs and symptoms of benign prostatic hyperplasia: a 9-month, open-label extension study. Urol 74:1318–1322

    PubMed  Google Scholar 

  • Marshall I, Burt RP, Chapple CR (1995) Noradrenaline contractions of human prostate mediated by α1A-(α1C-) adrenoceptor subtype. Br J Pharmacol 115:781–786

    CAS  PubMed  Google Scholar 

  • Martin DJ, Lluel P, Guillot E, Coste A, Jammes D, Angel I (1997) Comparative Alpha-1 adrenoceptor subtype selectivity and functional uroselectivity of Alpha-1 adrenoceptor antagonists. J Pharmacol Exp Ther 282:228–235

    CAS  PubMed  Google Scholar 

  • Maruyama K, Nakamura T, Yoshihara T, Fukutomi J, Sugiyama K, Hattorim K, Ohnuki T, Watanabe K, Nagatomo T (1998) Tamsulosin: assessment of affinity of 3H-prazosin bindings to two α1-adrenoceptor subtypes (α1H and α1L) in bovine prostate and rat heart and brain. Gen Pharmacol 31:597–600

    CAS  PubMed  Google Scholar 

  • Menon M, Parulkar BG, Drach DW (1998) Urinary lithiasis: etiology, diagnosis and medical management. In: Walsh PC, Retik AB, Vaughan ED, Wein AJ (eds) Campbell’s urology, vol 3, 7th edn. WB Saunders, Philadelphia, p 2702

    Google Scholar 

  • Michel MC (2010) The foreront for novel therapeutic agents based on the pathophysiology of lower urinary tract dysfunction: α-blocker in the treatment of male voiding dysfunction – how do they work and why do they differ in tolerability? J Pharmacl Sci 112:151–157

    CAS  Google Scholar 

  • Michel MC, de la Rosette JJ (2006) α-blocker treatment of urolithiasis. Eur Urol 50:213–214

    PubMed  Google Scholar 

  • Michel MC, Vrydag WV (2006) α1-, α2- and β-adrenoceptors in the urinary bladder, urethra and prostate. Br J Pharmacol 147:S88–S119

    CAS  PubMed  Google Scholar 

  • Michel MC, Grubbel B, Taguchi K, Verfurth F, Otto T, Kropfl D (1996) Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned α1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol 16:21–28

    CAS  PubMed  Google Scholar 

  • Milani S, Djavan B (2005) Lower urinary tract symptoms suggestive of benign prostatic hyperplasia: latest update on α1-adrenoceptor antagonists. BJU International 95(Suppl 4):29–36

    CAS  PubMed  Google Scholar 

  • Monneron MC, Gillberg PG, Ohman B, Alberts P (2000) In vitro α-adrenoceptor autoradiography of the urethra and urinary bladder of the female pig, cat, guinea-pig and rat. Scand J Urol Nephrol 34:233–238

    CAS  PubMed  Google Scholar 

  • Morita T, Wada I, Suzuki T, Tsuchida S (1987) Characterization of α-adrenoceptor subtypes involved in regulation of ureteral fluid transport. Tohoku J Exp Med 152:111–118

    CAS  PubMed  Google Scholar 

  • Morita T, Ando M, Kihara K, Oshima H (1994) Function and distribution of autonomic receptors in canine ureteral smooth muscle. Neurourol Urodyn 13:315–321

    CAS  PubMed  Google Scholar 

  • Muramatsu I, Ohmura T, Kigoshi S, Hashimoto S, Oshita M (1990) Pharmacological subclassification of α1-adrenoceptors in vascular smooth muscle. Br J Pharmacol 99:197–201

    CAS  PubMed  Google Scholar 

  • Nakamura Y, Tsujimoto G, Tanoue A, Ikegaki I, Shinozaki S, Nimura T, Matsuda Y, Kawatani M (2004) Is alpha-1D adrenergic receptor responsible for storage symptoms in mice?: effects of acetic acid on bladder function in mice lacking alpha-1D adrenergic receptor. Neurourol Urodyn 23:508

    CAS  Google Scholar 

  • Narayan P, O’Leary M, Davidai G (2005) Early efficacy of tamsulosin vs. terazosin in the treatment of men with benign prostatic hyperplasia: a randomized, open-label trial. J Appl Res 5:237–245

    Google Scholar 

  • Nasu K, Moriyama N, Kawabe K, Tsujimoto G, Murai M, Tanaka T, Yano J (1996) Quantification and distribution of α1-adrenoceptor subtype mRNAs in human prostate: comparison of benign hypertrophied tissue and non-hypertrophied tissue. Br J Pharmacol 119:797–803

    CAS  PubMed  Google Scholar 

  • Nasu K, Moriyama N, Fukasawa R, Tsujimoto G, Tanaka T, Yano J, Kawabe K (1998) Quantification and distribution of α1-adrenoceptor subtype mRNAs in human proximal urethra. Br J Pharmacol 123:1289–1293

    CAS  PubMed  Google Scholar 

  • Noble AJ, Chess-Williams R, Couldwell C, Furukawa K, Uchyiuma T, Korstanje C, Chapple CR (1997) The effects of tamsulosin, a high affinity antagonist at functional α1A- and α1B-adrenoceptor subtypes. Br J Pharmacol 120:231–238

    CAS  PubMed  Google Scholar 

  • Nomiya M, Yamaguchi O (2003) A quantitative analysis of mRNA expression of α1 and β-adrenoceptor subtypes and their functional roles in human normal and obstructed bladders. J Urol 170:649–653

    CAS  PubMed  Google Scholar 

  • Oesterling JE (1996) Benign prostatic hyperplasia: a review of its histogenesis and natural history. Prostate Suppl 6:67–73

    CAS  PubMed  Google Scholar 

  • Ohkura T, Yamada S, Deguchi Y, Kimura R, Matsushima H, Higuchi S, Inagaki O, Honda K, Takenaka T (1998) Ex vivo occupancy by tamsulosin of α1-adrenoceptors in rat tissues in relation to the plasma concentration. Life Sci 63:2147–2155

    CAS  PubMed  Google Scholar 

  • Ohkura T, Yamada S, Abe Y, Kimura R (2002) Selective and sustained occupancy of prostatic α1-adrenoceptors by oral administration of KMD-3213 and its plasma concentration in rats. J Pharm Pharmacol 54:975–982

    Google Scholar 

  • Ohmura T, Sakamoto S, Hayashi H, Kigoshi S, Muramatsu I (1993) Identification of α1-adrenoceptor subtypes in the dog prostate. Urol Res 21:211–215

    CAS  PubMed  Google Scholar 

  • Ohtake A, Ukai M, Saitoh C, Sonoda R, Noguchi Y, Okutsu H, Yuyama H, Sato S, Sasamata M, Miyata K (2006) Effect of tamsulosin on spontaneous bladder contraction in conscious rats with bladder outlet obstruction: comparison with effect on intraurethral pressure. Eur J Pharmacol 545:185–191

    CAS  PubMed  Google Scholar 

  • Okutsu H, Matsumoto S, Hanai T, Noguchi Y, Fujiyasu N, Ohtake A, Suzuki M, Sato S, Sasamata M, Uemura H, Kurita T (2010) Effects of tamsulosin on bladder blood flow and bladder function in rats with bladder outlet obstruction. Urol 75:235–240

    PubMed  Google Scholar 

  • Parsons JK, Hergan LA, Sakamoto K, Lakin C (2007) Efficacy of α-blockers for the treatment of urethral stones. J Urol 177:983–987

    CAS  PubMed  Google Scholar 

  • Pradidarcheep W, Stallen J, Labruyere WT, Dabhoiwala NF, Michel MC, Lamers WH (2009) Lack of specificity of commercially available antisera against muscarinergic and adrenergic receptors. Naunyn-Schmiedebergs Arch Pharmacol 379:397–402

    CAS  PubMed  Google Scholar 

  • Price DT, Schwinn DA, Lomasney JW, Allen LF, Caron MG, Lefkowitz RJ (1993) Identification, quantification, and localization of mRNA for three distinct alpha1 adrenergic receptor subtypes in human prostate. J Urol 150:546–551

    CAS  PubMed  Google Scholar 

  • Ramage AG, Wyllie MG (1995) A comparison of the effects of doxazosin and terazosin on the spontaneous sympathetic drive to the bladder and related organs in anaesthetized cats. Eur J Pharmacol 294:645–650

    CAS  PubMed  Google Scholar 

  • Sasaki S, Itoh Y, Kojima Y, Kubota Y, Hayase M, Kobayashi M, Tomiyama Y, Kobayashi S, Kohri K (2008) Expression level and role in ureteral contraction of alpha1-adrenoceptor subtypes in human ureter. Neurourol Urodyn 179(suppl):244

    Google Scholar 

  • Sato S, Ohtake A, Matsushima H, Saitoh C, Usuda S, Miyata K (2001) Pharmacological effect of tamsulosin in relation to dog plasma and tissue concentrations: prostatic and urethral retention possibly contributes to uroselectivity of tamsulosin. J Pharmacol Exp Ther 296:697–703

    CAS  PubMed  Google Scholar 

  • Schilit S, Benzeroual KE (2009) Silodosin: a selective alpha1A-adrenergic receptor antagonist for the treatment of benign prostatic hyperplasia. Clin Ther 31:2489–2502

    CAS  PubMed  Google Scholar 

  • Schulman CC (1974) Electron microscopy of the human ureteric innervation. Br J Urol 46:609–623

    CAS  PubMed  Google Scholar 

  • Schwinn DA (2001) The role of α1-adrenergic receptor subtypes in lower urinary tract symptoms. BJU Int 88(Suppl 2):27–34, discussion 49–50

    CAS  PubMed  Google Scholar 

  • Schwinn DA, Michelotti GA (2000) α1-Adrenergic receptors in the lower urinary tract and vascular bed: potential role for the alpha1d subtype in filling symptoms and effects of ageing on vascular expression. BJU Int 85(Suppl 2):6–11

    CAS  PubMed  Google Scholar 

  • Schwinn DA, Roehrborn CG (2008) α1-adrenoceptor subtypes and lower urinary tract symptoms. Int J Urol 15:193–199

    CAS  PubMed  Google Scholar 

  • Scofield MA, Liu F, Abel PW, Jeffries WB (1995) Quantification of steady state expression of mRNA for Alpha-1 adrenergic receptor subtypes using reverse transcription and a competitive polymerase chain reaction. J Pharmacol Exp Ther 275:1035–1042

    CAS  PubMed  Google Scholar 

  • Sigala S, Peroni A, Mirabella G, Fornari S, Palazzolo F, Pezzotti G, Simeone C, Cunico SC, Spano P (2004) Alpha1 adrenoceptor subtypes in human urinary bladder: sex and regional comparison. Life Sci 76:417–427

    CAS  PubMed  Google Scholar 

  • Sigala S, Dellabella M, Milanese G, Fornari S, Faccoli S, Palazzolo F, Peroni A, Mirabella G, Cunico SC, Spano P, Muzzonigro G (2005) Evidence for the presence of α1-adrenoceptor subtypes in the human ureter. Neurourol Urodyn 24:142–148

    CAS  PubMed  Google Scholar 

  • Smith MS, Schambra UB, Wilson KH, Page SO, Schwinn DA (1999) Alpha1-adrenergic receptors in human spinal cord: specific localized expression of mRNA encoding α1-adrenergic receptor subtypes at four distinct levels. Brain Res Mol Brain Res 63:254–261

    CAS  PubMed  Google Scholar 

  • Somogyi GT, Tanowitz M, de Groat WC (1995) Prejunctional facilitatory α1-adrenoceptors in the rat urinary bladder. Br J Pharmacol 114:1710–1716

    CAS  PubMed  Google Scholar 

  • Springer JP, Kropp BP, Thor KB (1994) Facilitatory and inhibitory effects of selective norepinephrine reuptake inhibitors on hypogastric nerve-evoked urethral contractions in the cat: a prominent role of urethral β-adrenergic receptors. J Urol 152:515–519

    CAS  PubMed  Google Scholar 

  • Sugaya K, Nishijima S, Miyazato M, Ashitomi K, Hatano T, Ogawa Y (2002) Effects of intrathecal injection of tamsulosin and naftopidil, alpha-1A and -1D adrenergic receptor antagonists, on bladder activity in rats. Neurosci Lett 328:74–76

    CAS  PubMed  Google Scholar 

  • Suzuki F, Miyamoto S, Takita M, Oshita M, Watanabe Y, Kakizuka A, Narumiya S, Taniguchi T, Muramatsu I (1997) Cloning, functional expression and tissue distribution of rabbit α1d-adrenoceptor. Biochim Biophys Acta 1323:6–11

    CAS  PubMed  Google Scholar 

  • Szell EA, Yamamoto T, de Groat WC, Somogyi GT (2000) Smooth muscle and parasympathetic nerve terminals in the rat urinary bladder have different subtypes of α1 adrenoceptors. Br J Pharmacol 130:1685–1691

    CAS  PubMed  Google Scholar 

  • Takeda H, Matsuzawa A, Igawa Y, Yamazaki Y, Kaidoh K, Akahane S, Kojima M, Miyata H, Akahane M, Nishizawa O (2003) Functional characterization of β-adrenoceptor subtypes in the canine and rat lower urinary tract. J Urol 170:654–658

    CAS  PubMed  Google Scholar 

  • Tatemichi S, Kobayashi K, Maezawa A, Kobayashi M, Yamazaki Y, Shibata N (2006) α1-Adrenoceptor subtype selectivity and organ specificity of silodosin (KMD-3213). Yakugaku Zasshi 126:209–216

    CAS  PubMed  Google Scholar 

  • Testa R, Guarneri L, Ibba M, Strada G, Poggesi E, Taddei C, Simonazzi I, Leonardi A (1993) Characterization of α1-adrenoceptor subtypes in prostate and prostatic urethra of rat, rabbit, dog and man. Eur J Pharmacol 249:307–315

    CAS  PubMed  Google Scholar 

  • Thor KB, Donatucci C (2004) Central nervous system control of the lower urinary tract: new pharmacological approaches to stress urinary incontinence in women. J Urol 172:27–33

    CAS  PubMed  Google Scholar 

  • Tiselius HG (2003) Epidemiology and medical management of stone disease. BJU Int 91:758–767

    PubMed  Google Scholar 

  • Tomiyama Y, Murakami M, Akiyama K, Kojima M, Akahane M, Park YC, Kurita T (2002) Modification of ureteral motility and promotion of urine flow around an intraureteral obstruction by CL-316243, phenylephrine, and furosemide in dogs. Neurourol Urodyn 21:251–257

    CAS  PubMed  Google Scholar 

  • Tomiyama Y, Kobayashi K, Tadachi M, Kobayashi S, Inada Y, Kobayashi M, Yamazaki Y (2007) Expressions and mechanical functions of α1-adrenoceptor subtypes in hamster ureter. Eur J Pharmacol 573:201–205

    CAS  PubMed  Google Scholar 

  • Trevisani M, Campi B, Gatti R, Andre E, Materazzi S, Nicoletti P, Gazzieri D, Geppetti P (2007) The influence of Alpha1-adrenoreceptors on neuropeptide release from primary sensory neurons of the lower urinary tract. Eur Urol 52:901–908

    CAS  PubMed  Google Scholar 

  • Tseng-Crank J, Kost T, Goetz A, Hazum S, Roberson KM, Haizlip J, Godinot N, Robertson CN, Saussy D (1995) The α1C-adrenoceptor in human prostate: cloning, functional expression, and localization to specific prostatic cell types. Br J Pharmacol 115:1475–1485

    CAS  PubMed  Google Scholar 

  • Tsujii T, Azuma H, Yamaguchi T, Oshima H (1992) A possible role of decreased relaxation mediated by β-adrenoceptors in bladder outlet obstruction by benign prostatic hyperplasia. Br J Pharmacol 107:803–807

    CAS  PubMed  Google Scholar 

  • Tzortzis V, Mamoulakis C, Rioja J, Gravas S, Michel MC, De la Rosette JJMCH (2009) Medical expulsive therapy for distal ureteral stones. Drugs 69:677–692

    CAS  PubMed  Google Scholar 

  • Walden PD, Durkin MM, Lepor H, Wetzel JM, Gluchowski C, Gustafson EL (1997) Localization of mRNA and receptor binding sites for the α1a-adrenoceptor subtype in the rat, monkey and human urinary bladder and prostate. J Urol 157:1032–1038

    CAS  PubMed  Google Scholar 

  • Walden PD, Gerardi C, Lepor H (1999) Localization and expression of the alpha1A-1, alpha1B and alpha1D-adrenoceptors in hyperplastic and non-hyperplastic human prostate. J Urol 161:635–640

    CAS  PubMed  Google Scholar 

  • Wanajo I, Tomiyama Y, Tadachi M, Kobayashi M, Yamazaki Y, Kojima M, Shibata N (2005) The potency of KUL-7211, a selective ureteral relaxant, in isolated canine ureter: comparison with various spasmolytics. Urol Res 33:409–414

    CAS  PubMed  Google Scholar 

  • Weiss RM, Bassett AL, Hoffman BF (1978) Adrenergic innervation of the ureter. Invest Urol 16:123–127

    CAS  PubMed  Google Scholar 

  • Wilde MI, Fitton A, McTavish D (1993a) Alfuzosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in benign prostatic hyperplasia. Drugs 45:410–429

    CAS  PubMed  Google Scholar 

  • Wilde MI, Fitton A, Sorkin EM (1993b) Terazosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in benign prostatic hyperplasia. Drugs Aging 3:258–277

    CAS  PubMed  Google Scholar 

  • Yamada S, Ashizawa N, Ushijima H, Nakayama K, Hayashi E, Honda K (1987) Alpha-1 adrenoceptors in human prostate: characterization and alteration in benign prostatic hypertrophy. J Pharmacol Exp Ther 242:326–330

    CAS  PubMed  Google Scholar 

  • Yamada S, Suzuki M, Matsuoka Y, Kato Y, Kimura R, Maruyama M, Kawabe K (1991) [3H]bunazosin, a novel selective radioligand of alpha 1 adrenoceptors in human prostates. J Urol 146:877–880

    CAS  PubMed  Google Scholar 

  • Yamada S, Suzuki M, Kato Y, Kimura R, Mori R, Matsumoto K, Maruyama M, Kawabe K (1992) Binding characteristics of naftopidil and alpha 1-adrenoceptor antagonists to prostatic alpha-adrenoceptors in benign prostatic hypertrophy. Life Sci 50:127–135

    CAS  PubMed  Google Scholar 

  • Yamada S, Suzuki M, Tanaka C, Mori R, Kimura R, Inagaki O, Honda K, Asano M, Takenaka T, Kawabe K (1994a) Comparative study on α1-adrenoceptor antagonist binding in human prostate and aorta. Clin Exp Pharmacol Physiol 21:405–411

    CAS  PubMed  Google Scholar 

  • Yamada S, Tanaka C, Kimura R, Kawabe K (1994b) Alpha 1-adrenoceptors in human prostate: characterization and binding characteristics of alpha 1-antagonists. Life Sci 54:1845–1854

    CAS  PubMed  Google Scholar 

  • Yamada S, Tanaka C, Ohkura T, Mori R, Kimura R, Inagaki O, Honda K, Kawabe K (1994c) High-affinity specific [3H]tamsulosin binding to alpha 1-adrenoceptors in human prostates with benign prostatic hypertrophy. Urol Res 22:273–278

    CAS  PubMed  Google Scholar 

  • Yamada S, Ohkura T, Kimura R, Kawabe K (1998) In vivo receptor binding of novel alpha1-adrenoceptor antagonists for treatment of benign prostatic hyperplasia. Life Sci 62:1585–1589

    CAS  PubMed  Google Scholar 

  • Yamada S, Ohkura T, Deguchi Y, Kimura R (1999) In vivo measurement by [3H]tamsulosin of alpha1 adrenoceptors in rat tissues in relation to the pharmacokinetics. J Pharmacol Exp Ther 289:1575–1583

    CAS  PubMed  Google Scholar 

  • Yamada S, Okura T, Kimura R (2001) In vivo demonstration of α1-adrenoceptor subtype selectivity of KMD-3213 in rat tissues. J Pharmacol Exp Ther 296:160–167

    CAS  PubMed  Google Scholar 

  • Yamagishi R, Akiyama K, Nakamura S, Hora M, Masuda N, Matsuzawa A, Murata S, Ujiie A, Kurashina Y, Iizuka K, Kitazawa M (1996) Effect of KMD-3213, an α1a-adrenoceptor-selective antagonist, on the contractions of rabbit prostate and rabbit and rat aorta. Eur J Pharmacol 315:73–79

    CAS  PubMed  Google Scholar 

  • Yazawa H, Honda K (1993) α1-adrenoceptor subtype in the rat prostate is preferentially the alpha 1A type. Jpn J Pharmacol 62:297–304

    CAS  PubMed  Google Scholar 

  • Yilmaz E, Batislam E, Basar MM, Tuglu D, Ferhat M, Basar H (2005) The comparison and efficacy of 3 difference α1-adrenergic blockers for distal ureteral stones. J Urol 173:2010–2012

    CAS  PubMed  Google Scholar 

  • Yokoyama O, Yusup A, Oyama N, Aoki Y, Tanase K, Matsuta Y, Miwa Y, Akino H (2006) Improvement of bladder storage function by α1-blocker depends on the suppression of C-fiber afferent activity in rats. Neurourol Urodyn 25:461–467

    CAS  PubMed  Google Scholar 

  • Yokoyama O, Yusup A, Oyama N, Aoki Y, Miwa Y, Akino H (2007) Improvement in bladder storage function by tamsulosin depends on suppression of C-fiber urethral afferent activity in rats. J Urol 177:771–775

    CAS  PubMed  Google Scholar 

  • Yono M, Foster HE Jr, Shin D, Takahashi W, Pouresmail M, Latifpour J (2004) Doxazosin-induced up-regulation of α1A-adrenoceptor mRNA in the rat lower urinary tract. Can J Physiol Pharmacol 82:872–878

    CAS  PubMed  Google Scholar 

  • Yoshimura N, Sasa M, Ohno Y, Yoshida O, Takaori S (1988) Contraction of urinary bladder by central norepinephrine originating in the locus coeruleus. J Urol 139:423–427

    CAS  PubMed  Google Scholar 

  • Yu SM, Ko FN, Chueh SC, Chen J, Chen SC, Chen CC, Teng CM (1994) Effects of dicentrine, a novel α1-adrenoceptor antagonist, on human hyperplastic prostates. Eur J Pharmacol 252:29–34

    CAS  PubMed  Google Scholar 

Download references

Acknowledgment

We express sincere thanks to Drs. Michel and Vrydag for referring to their excellent review article (Michel and Vrydag 2006).

Author information

Authors and Affiliations

  1. Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (GCOE) Program, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Shizuoka, 422-8526, Japan

    Shizuo Yamada & Yoshihiko Ito

Authors
  1. Shizuo Yamada
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Yoshihiko Ito
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Shizuo Yamada .

Editor information

Editors and Affiliations

  1. Wake Forest University, Medical Center Blvd., Winston-Salem, 27157-1088, North Carolina, USA

    Karl-Erik Andersson

  2. Academic Medical Center, Dept. Pharmacology & Pharmacotherapy, University of Amsterdam, Meibergdreef 15, Amsterdam, 1105 AZ, Netherlands

    Martin C. Michel

Rights and permissions

Reprints and permissions

Copyright information

© 2011 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

Yamada, S., Ito, Y. (2011). α1-Adrenoceptors in the Urinary Tract. In: Andersson, KE., Michel, M. (eds) Urinary Tract. Handbook of Experimental Pharmacology, vol 2011. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-16499-6_14

Download citation

Publish with us

Policies and ethics

Search

Navigation