RS-17053 (N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α, α-dimethyl-1H-indole-3-ethanamine hydrochloride), a selective α1A-adrenoceptor antagonist, displays low affinity for functional α1-adrenoceptors in human prostate: Implications for adrenoceptor classification

Molecular Pharmacology

Volumn 49, Issue 2, 1996, Pages 209-215

  Ford, Anthony P D W ^a   Arredondo, Nicolas F ^a   Blue Jr , David R ^a   Bonhaus, Douglas W ^a   Jasper, Jeffrey ^a   Kava, M Shannon ^a   Lesnick, John ^a   Pfister, Jurg R ^a,c   Shieh, I Amy ^a   Vimont, Rachel L ^a   Williams, Timothy J ^a   Mcneal, John E ^b   Stamey, Thomas A ^b   Clarke, David E ^a  

^a ROCHE BIOSCIENCE   (United States)

^b STANFORD UNIVERSITY MEDICAL CENTER   (United States)

^c CV THERAPEUTICS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 CHLORO 3 [2 [2 [2 (CYCLOPROPYLMETHOXY)PHENOXY]ETHYLAMINO] 2,2 DIMETHYLETHYL]INDOLE; 5 CHLORO N [2 (2 CYCLOPROPYLMETHOXYPHENOXY)ETHYL] ALPHA,ALPHA DIMETHYL 1H INDOLE 3 ETHANAMINE; ALPHA 1 ADRENERGIC RECEPTOR; ALPHA 1 ADRENERGIC RECEPTOR BLOCKING AGENT; CHLORIDE; CYSTEAMINE DERIVATIVE; PRAZOSIN; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ARTICLE; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; HUMAN TISSUE; NORADRENALIN RELEASE; PRIORITY JOURNAL; RECEPTOR AFFINITY; SMOOTH MUSCLE CONTRACTION;

ADRENERGIC ALPHA-ANTAGONISTS; ANIMALS; BINDING, COMPETITIVE; CATTLE; CRICETINAE; HUMANS; INDOLES; KINETICS; MALE; MUSCLE CONTRACTION; MUSCLE, SMOOTH; NOREPINEPHRINE; PROSTATE; RADIOLIGAND ASSAY; RATS; RECEPTORS, ADRENERGIC, ALPHA-1; URINARY TRACT; URINARY TRACT PHYSIOLOGY;

EID: 0030046789     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (26)

1. 1-Adrenoceptor classification: sharpening Occam's razor. Trends Pharmacol. Sci. 15:167-170 (1994).
2. 1-adrenoceptors. Pharmacol. Rev. 47:267-270 (1995).
3. Holck, C M., C H. M. Jones, and G. Haeusler. Differential interactions of clonidine and methoxamine with postsynaptic α-adrenoceptors of rabbit main pulmonary artery. Cardiovasc. Res. 5:240-248 (1983).
4. Flavahan, N. A., and P. M. VanHoutte. α-Adrenoceptor classification in vascular smooth muscle. Trends Pharmacol. Sci. 7:347-349 (1986).
5. 1-adrenoceptors: subclassification and functional aspects, in α-Adrenoceptors (Fujiwara, M., Sugimoto, T., and Kogure, K., eds.). Excerpta Medica Ltd., Tokyo, 193-202 (1992).
6. 1-adrenergic receptor subtypes in human prostate J. Urol. 150:546-551 (1993).
7. 1C-adrenoceptor subtype. Mol. Pharmacol. 45:703-708 (1994).
8. 1-adrenoceptor subtypes present in the human prostate. Life Sci. 54:1595-1605 (1994).
9. 1C-adrenoeeptor functional characterisation in prostate. Br J. Pharmacol. 112:59P (1992).
10. 1C-)adrenoceptor subtype. Br. J. Pharmacol. 115:781-786 (1995).
11. 1-adrenoceptor subtypes mediating the contraction of human prostatic urethra and peripheral artery. Br. J. Pharmacol. 113:723-728 (1994).
12. 1-adrenoceptor subtypes in the human prostate: functional and binding studies. Br. J. Urol. 74:572-577 (1994).
13. 2+ channel antagonist niguldipine. J. Med. Chem. 38:1879-1581 (1995).
14. 1-adrenoceptors. Eur. J. Pharmacol. 172:131-145 (1989).
15. 1A-AR antagonist, RS-17053. Br. J. Pharmacol 114:24P 1995
16. 1C-adrenoceptors: studies in the isolated perfused kidney of rat Br. J. Pharmacol. 115:283-294 (1995).
17. 1) and the concentration of inhibitor which causes 50 percent inhibition of an enzymatic reaction. Biochem. Pharmacol. 22:3099-3108 (1973).
18. 1-adrenoceptors mediating vasoconstriction to noradrenaline and nerve stimulation in the isolated perfused mesentery of rat. Br. J. Pharmacol. 114:531-536 (1995).
19. Jenkinson, D H., E. A. Barnard, D. Hoyer, P. P. A. Humphrey, P. Leff, and N. P. Shankley. International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. IX Recommendations on terms and symbols in quantitative pharmacology. Pharmacol. Rev. 47: 255-266 (1995).
20. 1-adrenoceptors. Eur. J. Pharmacol. 272:R5-R6 (1995).
21. 1D-adrenoceptor antagonist, isolated from Fissistigma glaucescens. Br. J. Pharmacol. 112:1174-1179 (1994).
22. 1D subtype. Can. J. Physiol. Pharmacol. 72(Suppl.):323 (1994).
23. 1D-adrenoeeptor in rat aorta. Br. J. Pharmacol. 114:25P (1995).
24. 1A-adrenoceptor in caudal artery of rat. Br. J. Pharmacol. 116:300P (1995).
25. 1-adrenoceptors in isolated anococcygeus muscle of rat. Br J. Pharmacol 109:P112 (1993).
26. 1C-adrenoceptor splice variants. FEBS Lett. 363:256-260 (1995).