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Nicotinic acetylcholine receptors in the rat stomach: I. (-)-[3H]nicotine binding.

Abstract：

:The nicotinic acetylcholine receptors in the rat stomach were characterized by means of a radioligand binding assay with (-)-[3H]nicotine as ligand. Saturation binding studies on the gastric fundus membranes revealed the presence of two binding sites with dissociation constant (KD) values of 3.1 and 289 nM, and maximum binding capacity (Bmax) values of 3.6 and 76 fmol/mg protein, respectively. The Bmax of the high affinity binding site was greatest in the cardia, followed by fundal mucosa, fundal muscle, and, finally antrum. The IC50 values of cholinergic drugs to inhibit (-)-[3H]nicotine binding in fundus membranes were as follows: (-)nicotine, 0.12 nM; cytosine, 9.3 nM; acetylcholine, 17.7 nM; carbachol, 700 nM; hexamethonium, 2270 nM. The IC50 values of alpha-bungarotoxin, d-tubocurarine and atropine were greater than 100 microM. The muscarinic acetylcholine receptors were also characterized with [3H]quinuclidinyl benzilate and the choline acetyltransferase activity was measured. These results suggest that nicotinic acetylcholine receptors as well as muscarinic acetylcholine receptors are present in the rat stomach and that the regional distribution of these receptors is uneven.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Nishikawa H,Taniguchi T,Ninomiya H,Fujiwara M

doi

10.1016/0014-2999(88)90490-6

subject

Has Abstract

pub_date

1988-01-27 00:00:00

pages

97-103

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(88)90490-6

journal_volume

146

pub_type

杂志文章

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