| Title |
Preferential action of eptazocine, a novel analgesic, with opioid receptors in isolated guinea pig ileum and mouse vas deferens preparations
|
|---|---|
| Published in |
Folia Pharmacologica Japonica, January 1990
|
| DOI | 10.1254/fpj.95.1_41 |
| Pubmed ID | |
| Authors |
T Tamura, J Ogawa, T Taniguchi, I Waki |
| Abstract |
Actions of eptazocine, a novel analgesic, on isolated smooth muscle preparations were investigated. Eptazocine (10(-5) M) slightly inhibited electrically-driven twitch-tension in guinea pig ileum preparations sensitive to mu- and kappa-agonists, and this effect was antagonized by 10(-7) M naloxone. Eptazocine (10(-5)-10(-4) M) inhibited such an effect by the mu-agonist morphine. In mouse vas deferens preparations having delta-, mu- and kappa-receptors, eptazocine (10(-7) M-) inhibited the twitch-tension in a dose-dependent manner, being hardly inhibited by naloxone. On the other hand, MR-2266 (10(-6) M), a relatively selective kappa-receptor antagonist, inhibited the eptazocine effect. The Ke (equilibrium dissociation constant) value of naloxone against eptazocine was 325 nM and the Ke value of MR-2266 against eptazocine was 33.2 nM, showing that MR-2266 was 9.79-fold more effective than naloxone. These results suggest that eptazocine acted as a mu-receptor antagonist and as a kappa-receptor preferential agonist in isolated smooth muscle preparations. |
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Attention Score in Context
This research output has an Altmetric Attention Score of 3. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 01 September 2016.
All research outputs
#7,454,951
of 22,790,780 outputs
Outputs from Folia Pharmacologica Japonica
#189
of 783 outputs
Outputs of similar age
#11,388
of 58,043 outputs
Outputs of similar age from Folia Pharmacologica Japonica
#2
of 9 outputs
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