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A comparison of the relative activities of a number of GABAB antagonists in the isolated vas deferens of the rat.

Abstract：

:1. A series of GABAB receptor antagonists were tested against (+/-)-baclofen for activity on the presynaptic GABAB receptor in the rat vas deferens. 2. All the antagonists tested caused a rightward shift in the concentration-response curve to (+/-)-baclofen. 3. pA2 values calculated from full Schild analysis were as follows: phaclofen, pA2 = 4.3; delta-amino valeric acid, pA2 = 4.4; 3-aminopropyl(diethoxymethyl)phosphinic acid (CGP 35348), pA2 = 5.0; 3-amino-propyl(n-hexyl)phosphinic acid (3-APHPA), pA2 = 4.5. 4. These results show that none of the above compounds possess potent antagonist activity at the GABAB receptor (i.e. pA2 > 6) in this peripheral tissue. In addition, the more recently available phosphinic acid antagonists, appear to offer no great advance over the GABAB antagonists previously available.

journal_name

Br J Pharmacol

journal_title

British journal of pharmacology

authors

Hills JM,Larkin MM,Howson W

doi

10.1111/j.1476-5381.1991.tb12224.x

subject

Has Abstract

pub_date

1991-03-01 00:00:00

pages

631-4

issue

3

eissn

0007-1188

issn

1476-5381

journal_volume

102

pub_type

杂志文章

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