Effects of BAM-22P, an opioid peptide derived from proenkephalin A, on in vitro isolated preparations

In the presence of peptidase inhibitors, BAM-22P was approximately five-fold less potent than 「Met^5 」-enkephalin in hamster vas deferens which contained δ-receptors alone, while it was about three-fold less potent than dynorphin-(1-8) in rabbit vas deferens which contained only κ-receptors. Additio...

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Bibliographic Details
Published in:Japanese Journal of Pharmacology 1994, Vol.64 (suppl.1), p.192-192
Main Authors: Iwao, Kayoko, Matsumiya, Teruhiko, Kitamura, Ken, Fan, Xintian, Tominaga, Keiko, Ohgiya, Nobuyuki, Oka, Tetsuo
Format: Article
Language:eng ; jpn
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Summary:In the presence of peptidase inhibitors, BAM-22P was approximately five-fold less potent than 「Met^5 」-enkephalin in hamster vas deferens which contained δ-receptors alone, while it was about three-fold less potent than dynorphin-(1-8) in rabbit vas deferens which contained only κ-receptors. Additionally, BAM-22P was approximately ten-fold more potent than 「Met^5 」-enkephalin in guinea-pig ileum in which it was suggested by the Ke value of CTOP, a selective μ-antagonist, to act mainly on μ-receptors. However, the Ke value of CTOP indicated that BAM-22P did not selectively act on μ-receptors in mouse vas deferens. In conclusion, BAM-22P was indicated in the present study to be a non-selective agonist with low, intermediate, or high potency at δ-, κ-, or μ-opioid receptor sites, respectively.
ISSN:0021-5198
DOI:10.1016/S0021-5198(19)50401-2