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- W1994843652 abstract "1 Virginiamycin, a macrolide reported to bind selectively to CCKB/gastrin receptors has been studied in a functional test, namely cholecystokinin-induced contraction of guinea-pig ileum myenteric plexus (LMMP). 2 Virginiamycin (1–10 μm) antagonized the selective CCKB agonist cholecystokinin tetrapeptide (CCK-4). The antagonism appeared not to be competitive as the highest concentration (10 μm) caused a reduction of its maximal effect. An apparent pA2 of 6.64 ± 0.06 (s.e.) could be estimated if this depression was ignored. The selective CCKB antagonist, L-365,260 (0.01–0.3 μm) antagonized competitively the CCK-4 induced contraction and a pKB of 8.60 ± 0.16 (s.e.) was estimated. 3 The combined dose-ratio analysis for virginiamycin, tested at 3 and 10 μm in association with 0.03 and 0.1 μm L-365,260, respectively, resulted in observed log dose-ratios of 1.39 and 1.53. That was consistent with both antagonists acting on the same receptor in LMMP. 4 These data, represent the first evidence of the antagonism of virginiamycin in a functional assay and they support the hypothesis of homogeneity between CCKB receptors in the CNS and in peripheral tissues." @default.
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- W1994843652 date "1993-04-01" @default.
- W1994843652 modified "2023-09-25" @default.
- W1994843652 title "Analysis of the CCKB receptor antagonism of virginiamycin in guinea-pig ileum longitudinal myenteric plexus" @default.
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- W1994843652 doi "https://doi.org/10.1111/j.1476-5381.1993.tb13521.x" @default.
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