ADENOSINE-A(3) RECEPTORS MEDIATE HYPOTENSION IN THE ANGIOTENSIN II-SUPPORTED CIRCULATION OF THE PITHED RAT

被引：119

作者：

FOZARD, JR

CARRUTHERS, AM

机构：

[1] Preclinical Research, Sandoz Pharma Ltd., Basel

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 1993年 / 109卷 / 01期

关键词：

5'-N-ETHYLCARBOXAMIDOADENOSINE (NECA); R-N-6-PHENYLISOPROPYLADENOSINE (R-PIA); S-N-6-PHENYLISOPROPYLADENOSINE (S-PIA); N-6-2-(4-AMINOPHENYL)ETHYL ADENOSINE (APNEA); HYPOTENSION; A3-ADENOSINE RECEPTORS;

D O I：

10.1111/j.1476-5381.1993.tb13522.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The cardiovascular effects of N6-2-(4-aminophenyl)ethyladenosine (APNEA), which when radiolabelled with I-125 shows high affinity for the newly described adenosine A3 receptor, have been investigated in the angiotension II-supported circulation of the pithed rat. APNEA induces hypotensive responses which are unaffected by high doses (20-40 mg kg-1) of the broad spectrum, adenosine receptor antagonist, 8-(p-sulphophenyl)theophylline (8-SPT). 8-SPT-resistant falls in blood pressure are also seen, in the absence of bradycardia, with 5'-N-ethylcarboxamidoadenosine (NECA) and the R-and S-enantiomers of N6-phenylisopropyladenosine (PIA). Xanthine insensitivity, high potencies of APNEA, NECA and R-PIA, and an enantiomeric selectivity favouring R- over S-PIA are distinguishing features of the adenosine A3 receptor. We suggest that hypotension in the pithed rat may be a functional correlate of this site.

引用

页码：3 / 5

页数：3

共 9 条

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[2]

CARRUTHERS AM, 1992, BRIT J PHARMACOL, V106, pP94

[3]

FOZARD JR, 1993, IN PRESS NAUNYNSCHMI

[4]

HARGREAVES MB, 1990, BRIT J PHARMACOL, V102, pP198