Abstract：
:The characteristics of the muscarinic receptor in isolated gastric fundic cells from rabbit were determined by radioligand binding techniques and functional tests. The dissociation constants (KDS) of selective (hexahydrosiladifenidol and pirenzepine) and non-selective (N-methylscopolamine and atropine) muscarinic receptor antagonists obtained in competition experiments vs [3H]-N-methylscopolamine were compared with the pA2 values of the drugs as inhibitors of carbachol-stimulated [14C]-aminopyrine accumulation (an index of acid secretion) in the gastric fundic cells. Good correlations were found between the ability of the drugs to inhibit acid secretion and their affinity for muscarinic receptors in the gastric fundic cells. The rank order of potency in both tests was N-methylscopolamine greater than atropine greater than hexahydrosiladifenidol greater than pirenzepine. The character of the muscarinic receptor subtype present on gastric fundic cells was established by comparing the affinity values of the compounds for this receptor with those for the receptors in other rabbit tissues. It was found that only pirenzepine and hexahydrosiladifenidol displayed tissue selectivity in their binding profiles. The KDS for pirenzepine were 13nM for the M1 receptor of the cerebral cortex and about 500 nM for the M2 receptors of the submandibular and gastric glands and heart. Differently from pirenzepine, hexahydrosiladifenidol showed about 10-fold discrimination between the M2 subtype of the gland (KD = 31 nM) and the M2 subtype of the heart (KD = 330 nM).
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Baudiere B,Monferini E,Giraldo E,Ladinsky H,Bali JPdoi
10.1016/0006-2952(87)90209-7subject
Has Abstractpub_date
1987-09-15 00:00:00pages
2957-61issue
18eissn
0006-2952issn
1873-2968pii
0006-2952(87)90209-7journal_volume
36pub_type
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pub_type： 杂志文章
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更新日期：1987-03-15 00:00:00
