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|Title: ||α1-Adrenoceptor subtypes in isolated corporal tissue from patients undergoing gender re-assignment|
|Authors: ||El-Gamal, Osama M.|
Sandhu, Davinder P.S.
Elliott, Ruth A.
|Issue Date: ||Feb-2006|
|Citation: ||BJU International, 2006, 97 (2), pp. 329-332.|
To investigate the pharmacology and functionality of α1-adrenoceptors in human corpus cavernosum, and to determine the predominant subtype.
MATERIALS AND METHODS:
Cavernosal tissue specimens were obtained from the penises of 22 men (mean age 37.4 years) removed during gender re-assignment surgery. The men had been maintained on long-term oestrogen therapy before surgery, to aid the development of secondary feminine characteristics (oestrogen treatments were stopped 6 weeks before surgery). Corpus cavernosum strips were mounted in organ baths perfused with Krebs’ solution. A control concentration-response curve (CRC) to phenylephrine (a nonselective α1-agonist) was obtained. Then the tissues were incubated with the α1A antagonist, WB4101; the α1B antagonist, chloroethylclonidine; or the α1D antagonist BMY 7378 (all at 1 µM) and the CRC to phenylephrine was repeated. The concentration producing a half-maximal response (EC50) and pKB values (logarithm of the dissociation constant, a measure of affinity) were determined.
WB4101 produced a parallel rightward shift of the CRC to phenylephrine, with a pKB of 7.49. BMY 7378 also produced a parallel rightward shift of the CRC to phenylephrine with a pKB of 6.45. Chloroethylclonidine had a similar effect on the phenylephrine CRC, with a pKB of 5.90.
α1-adrenoceptors in human cavernosal tissue have a relatively low affinity for BMY 7378 and chloroethylclonidine, but are more sensitive to WB4101. This confirms that the predominant α1-adrenoceptor subtype in human corpus cavernosum is the α1A subtype and this might help in developing more selective antagonists and agonists for managing erectile dysfunction and priapism.|
|Description: ||This paper was published as BJU International, 2006, 97 (2), pp. 329-332. It is available from http://onlinelibrary.wiley.com/journal/10.1111/(ISSN)1464-410X. Doi: 10.1111/j.1464-410X.2006.05956.x|
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|Appears in Collections:||Published Articles, Dept. of Cancer Studies and Molecular Medicine|
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