Two district alpha(1)-adrenoceptor subtypes in the human prostate: assessment by radioligand binding assay using 3H-prazosin.
1. We showed that there were two distinct alpha(1)-adrenoceptor subtypes (alpha(1H) and alpha(IL)) in the human prostate which show different affinities for 3H-prazosin. 2. WB4101, tamsulosin, 5-methylurapizil, phentolamin, and terazosin, but not nifedipine, had significantly higher pKi values for the alpha(1H)-subtype than for the alpha(IL)-subtypes. 3. There was good correlation (r = 0.92, P < 0.05) between the pKi values obtained for the alpha(1H)-receptors in membrane fractions and the cloned human alpha(1c)-adrenoceptor subtype.
Maruyama
K
K
Department of Pharmacology, Niigata College of Pharmacy, Japan.
Fukutomi
J
J
Chiba
T
T
Yamaguchi
M
M
Takeda
M
M
Hattori
K
K
Nagatomo
T
T
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000378:metabolism*; D001667:Binding, Competitive / Q000187:drug effects; D004146:Dioxanes / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D009543:Nifedipine / Q000378:metabolism; D010646:Phentolamine / Q000378:metabolism; D010879:Piperazines / Q000378:metabolism / Q000494:pharmacology; D011224:Prazosin / Q000031:analogs & derivatives / Q000378:metabolism*; D011467:Prostate / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding / Q000187:drug effects; D011869:Radioligand Assay; D018340:Receptors, Adrenergic, alpha-1 / Q000145:classification* / Q000378:metabolism; D013449:Sulfonamides / Q000378:metabolism; D000077409:Tamsulosin; D014316:Tritium
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D004146:Dioxanes; D010879:Piperazines; D018340:Receptors, Adrenergic, alpha-1; D013449:Sulfonamides; D014316:Tritium; C057446:5-methylurapidil; C041226:Terazosin; C010654:(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane; D000077409:Tamsulosin; D009543:Nifedipine; D011224:Prazosin; D010646:Phentolamine