Abstract:
:The effects of the d- and l-isomers of pentazocine were compared to that of racemic pentazocine on contractions of the mouse isolated vas deferens. L-pentazocine inhibited electrically evoked contractions of the mouse vas deferens (MVD) in a dose-dependent manner (ID50 0.37 +/- 0.04 microM). In contrast, d-pentazocine augmented field stimulated contractions dose-dependently; per cent increases in contractions at 10 and 30 microM were 57.8 +/- 18.0 and 98.0 +/- 15.1%, respectively. Racemic pentazocine produced an intermediate effect between the two isomers. The effect of 1-pentazocine was antagonized by naloxone, whereas that of d-pentazocine was not. L-pentazocine did not effect the response of the MVD to exogenous norepinephrine at any concentration tested, while d-pentazocine depressed the response of the MVD to exogenous norepinephrine at one dose (0.3 microM). These findings demonstrate that d- and l-pentazocine produce opposite effects on the MVD. The effects of l-pentazocine are opioid mediated, while those of d-pentazocine are not. In the racemic mixture the opposing effects of the two isomers modulate each other, resulting in a diminished effect.
journal_name
Life Scijournal_title
Life sciencesauthors
Kinouchi K,Fukumitsu K,Takezawa J,Maeda S,Enomoto H,Kakuhari J,Yoshiya I,Inoki Rdoi
10.1016/0024-3205(86)90446-7subject
Has Abstractpub_date
1986-07-14 00:00:00pages
127-33issue
2eissn
0024-3205issn
1879-0631pii
0024-3205(86)90446-7journal_volume
39pub_type
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