Synthesis of a selective alpha-2A adrenoceptor antagonist, BRL 48962, and its characterization at cloned human alpha-adrenoceptors

被引：11

作者：

Beeley, LJ

Berge, JM

Chapman, H

Hieble, P

Kelly, J

Naselsky, DP

Rockell, CM

Young, PW

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,EPSOM KT18 5XQ,SURREY,ENGLAND

[2] SMITHKLINE BEECHAM PHARMACEUT,DEPT VASC BIOL,WELWYN GARDEN CIT AL6 9AR,HERTS,ENGLAND

[3] SMITHKLINE BEECHAM PHARMACEUT,DEPT PHARMACOL,KING OF PRUSSIA,PA 19406

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1995年 / 3卷 / 12期

关键词：

D O I：

10.1016/0968-0896(95)00157-3

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The chiral synthesis of the potent and selective alpha-2A antagonist, BRL 48962, is described. Evaluation of BRL 48962 at cloned human alpha-adrenoceptors indicates that this antagonist has a selectivity in the order of 30-fold for the alpha-2A subtype.

引用

页码：1693 / 1698

页数：6

共 25 条

[1] SOME QUANTITATIVE USES OF DRUG ANTAGONISTS
ARUNLAKSHANA, O
SCHILD, HO
[J]. BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1959, 14 (01): : 48 - 58
[2] NOVEL 1-SUBSTITUTED-2,3-DIHYDRO-1H-ISOINDOLES - SYNTHESIS VIA MEYERS METHODOLOGY
BEELEY, LJ
ROCKELL, CJM
[J]. TETRAHEDRON LETTERS, 1990, 31 (03) : 417 - 420
[3] BEELEY LJ, 1991, 8TH TRENDS REC RES C
[4] LOCALIZATION OF MESSENGER-RNA FOR 3 DISTINCT ALPHA(2)-ADRENERGIC RECEPTOR SUBTYPES IN HUMAN TISSUES - EVIDENCE FOR SPECIES HETEROGENEITY AND IMPLICATIONS FOR HUMAN PHARMACOLOGY
BERKOWITZ, DE
PRICE, DT
BELLO, EA
PAGE, SO
SCHWINN, DA
[J]. ANESTHESIOLOGY, 1994, 81 (05) : 1235 - 1244
[5] FUNCTIONAL BASIS FOR CLASSIFICATION OF ALPHA-ADRENERGIC RECEPTORS
BERTHELSEN, S
PETTINGER, WA
[J]. LIFE SCIENCES, 1977, 21 (05) : 595 - 606
[6] FACILE SYNTHESIS OF DIHYDROISOINDOLE
BORNSTEIN, J
LASHUA, SC
BOISSELLE, AP
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1957, 22 (10) : 1255 - 1256
[7] BYLUND DB, 1992, MOL PHARMACOL, V42, P1
[8] HETEROGENEITY OF ALPHA-2 ADRENERGIC-RECEPTORS
BYLUND, DB
[J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1985, 22 (05) : 835 - 843
[9] SMOOTH-MUSCLE OF RABBIT AORTA CONTAINS ALPHA-1-ADRENOCEPTORS BUT NOT ALPHA-2-ADRENOCEPTORS
DOCHERTY, JR
CONSTANTINE, JW
STARKE, K
[J]. NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1981, 317 (01) : 5 - 7
[10] ALPHA-1-ADRENOCEPTOR CLASSIFICATION - SHARPENING OCCAM RAZOR
FORD, APDW
WILLIAMS, TJ
BLUE, DR
CLARKE, DE
[J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1994, 15 (06) : 167 - 170

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