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Review
. 2006 Feb;147 Suppl 2(Suppl 2):S88-119.
doi: 10.1038/sj.bjp.0706619.

Alpha1-, alpha2- and beta-adrenoceptors in the urinary bladder, urethra and prostate

Martin C Michel  1 , Wim Vrydag
Affiliations
Review

Alpha1-, alpha2- and beta-adrenoceptors in the urinary bladder, urethra and prostate

Martin C Michel et al. Br J Pharmacol. 2006 Feb.

Abstract

1 We have systematically reviewed the presence, functional responses and regulation of alpha(1)-, alpha(2)- and beta-adrenoceptors in the bladder, urethra and prostate, with special emphasis on human tissues and receptor subtypes. 2 Alpha(1)-adrenoceptors are only poorly expressed and play a limited functional role in the detrusor. Alpha(1)-adrenoceptors, particularly their alpha(1A)-subtype, show a more pronounced expression and promote contraction of the bladder neck, urethra and prostate to enhance bladder outlet resistance, particularly in elderly men with enlarged prostates. Alpha(1)-adrenoceptor agonists are important in the treatment of symptoms of benign prostatic hyperplasia, but their beneficial effects may involve receptors within and outside the prostate. 3 Alpha(2)-adrenoceptors, mainly their alpha(2A)-subtype, are expressed in bladder, urethra and prostate. They mediate pre-junctional inhibition of neurotransmitter release and also a weak contractile effect in the urethra of some species, but not humans. Their overall post-junctional function in the lower urinary tract remains largely unclear. 4 Beta-adrenoceptors mediate relaxation of smooth muscle in the bladder, urethra and prostate. The available tools have limited the unequivocal identification of receptor subtypes at the protein and functional levels, but it appears that the beta(3)- and beta(2)-subtypes are important in the human bladder and urethra, respectively. Beta(3)-adrenoceptor agonists are promising drug candidates for the treatment of the overactive bladder. 5 We propose that the overall function of adrenoceptors in the lower urinary tract is to promote urinary continence. Further elucidation of the functional roles of their subtypes will help a better understanding of voiding dysfunction and its treatment.

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Figures

Figure 1
Figure 1
Presence of α1A-adrenoceptor protein in the lower urinary tract of the monkey. Receptors were localized by autoradiography, using [3H]praozsin and defining non-specific binding in the presence of SNAP 5272. Receptor autoradiograms were scanned into computer as a 16 grey scale image. The 16 grey levels corresponding to specific α1A-adrenoceptor receptor binding were each assigned colour (see scale) to allow subtle differences in film exposure to be easily visible. Sections show bladder dome and prostate (i), bladder trigone (ii), bladder base (iii), prostatic urethra (iv) and penile urethra (v). Key: sm (smooth muscle); ur (urothelium); lm (longitudinal muscle). Schematic representation of monkey urinary tract together with the orientation of sectioning planes (i)–(v) shown in (b). Taken with permission from Walden et al. (1997).
Figure 2
Figure 2
Inhibition of isoprenaline-induced relaxation of human bladder detrusor by the β1-antagonist CGP 20,712, the β2-antagonist ICI 118,551 and the nonselective antagonist SR 58,894. Taken with permission from Igawa et al. (1999).
Figure 3
Figure 3
Competition of subtype-selective antagonists for [3H]prazosin binding to human prostate membranes. Data are means of 4–5 experiments (error bars deleted for clarity). Modified with permission from Michel et al. (1996).
Figure 4
Figure 4
Potency and affinity of prazosin and tamsulosin at cloned α1A-adrenoceptors and those in human and rabbit prostate. Data are from individual studies (filled circles) and their means (horizontal lines), and given as pKi (binding studies) or pKB/pA2 (functional studies), as taken from the following references: Hieble et al. (1985); Chapple et al. (1989); Morita & Kondo (1992a); Yamada et al. (1992); Lefevre-Borg et al. (1993); Testa et al. (1993; 1996); Faure et al. (1994); Forray et al. (1994); Goetz et al. (1994); Teng et al. (1994); Yu et al. (1994); Hancock et al. (1995); Marshall et al. (1995); Tseng-Crank et al. (1995); Chueh et al. (1996); Ford et al. (1996); Hatano et al. (1996); Kenny et al. (1996); Michel et al. (1996); Leonardi et al. (1997); Martin et al. (1997); Noble et al. (1997); Chang et al. (2000).
Figure 5
Figure 5
α1A-Adrenoceptor mRNA (upper panel) and total α1-adrenoceptor protein expression (lower panel) in prostates from BPH patients. Data are expressed as % of the corresponding control group and taken from Chapple et al. (1989); Gup et al. (1990); Tsujii et al. (1992); Nasu et al. (1996); Moriyama et al. (1998). *P<0.05 vs control in the respective study. Note that Moriyama et al. have studied the urethral, central and peripheral zones in parallel.
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