Topic
Benzomorphans
About: Benzomorphans is a research topic. Over the lifetime, 165 publications have been published within this topic receiving 2435 citations.
Papers published on a yearly basis
Papers
TL;DR: Four benzomorphans which have potent antinociceptive activity in the hot‐plate and writhing tests in the mouse but do not suppress or precipitate withdrawal symptoms in the morphine‐dependent monkey, have been examined for their pharmacological actions in the guinea‐pig ileum and mouse vas deferens.
Abstract: 1 Four benzomorphans which have potent antinociceptive activity in the hot-plate and writhing tests in the mouse but do not suppress or precipitate withdrawal symptoms in the morphine-dependent monkey, have been examined for their pharmacological actions in the guinea-pig ileum and mouse vas deferens 2 In the guinea-pig ileum their agonist potencies are 15 to 400 times greater than that of normorphine of morphine whereas in the mouse vas deferens their potencies relative to morphine are 03 to 100 They exhibit no antagonist activity in either preparation Benzomorphans which substitute for morphine in the morphine-dependent monkey do not show such differences between their relative potencies in the guinea-pig ileum and mouse vas diferens 3 The relative potencies of the four benzomorphans to inhibit stereospecific [3H]-dihydromorphine binding by membrane fragments from rat brain, are more closely related to their relative agonist potencies in the mouse vas deferens than to those found in the guinea-pig ileum 4 In order to antagonize the agonist actions of these benzomorphans, naloxone is required in concentrations which are 3 to 7 times higher than those needed for the antagonism of normorphine or morphine or of benzomorphans which suppress abstinence in morphine-dependent monkeys 5 It may be possible to use the three assays, namely, ratio of relative agonist potency in mouse vas deferens to that in guinea-pig ileum, ratio of relative agonist potency to relative affinity to opiate receptors and the concentration of nalozone required for antagonism, for the prediction of the potential of new compounds to produce physical dependence
186 citations
108 citations
TL;DR: The benzomorphans, ethylketazocines, bremazocine and MR 2034 are pure agonists in the guinea‐pig ileum and mouse vas deferens but are competitive antagonists without agonist activity in the rat vas deferenns.
Abstract: The benzomorphans, ethylketazocine, bremazocine and MR 2034 are pure agonists in the guinea-pig ileum and mouse vas deferens but are competitive antagonists without agonist activity in the rat vas deferens.
82 citations
TL;DR: It is concluded that actions at s‐ but not κ‐, opiate receptors are responsible for the NMA antagonism observed with benzomorphans.
Abstract: Using the technique of microelectrophoresis in pentobarbitone-anaesthetized cats and rats, the effects of benzomorphans, with known actions at sigma- and kappa- opioid receptors, were tested on responses of spinal neurones to amino acids and acetylcholine. The racemic mixture and both enantiomers of the sigma opiate receptor agonist, N-allylnormetazocine (SKF 10, 047), and the dissociative anaesthetic, ketamine, reduced or abolished excitation evoked by N-methyl-aspartate (NMA) with only small and variable effects on responses to quisqualate or kainate. (+)-SKF 10, 047 was 1.2 +/- 0.7 times more potent than the (-)-enantiomer in antagonizing NMA. On Renshaw cells, (+)-SKF 10, 047 enhanced responses to acetylcholine whereas the (-) enantiomer produced only a small reduction. The kappa- opiate receptor agonist, ethylketocyclazocine, had no selective effects on responses to amino acids or to acetylcholine. We conclude that actions at sigma- but not kappa-, opiate receptors are responsible for the NMA antagonism observed with benzomorphans.
82 citations
73 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2020 | 1 |
| 2016 | 1 |
| 2011 | 2 |
| 2010 | 1 |
| 2009 | 1 |
| 2008 | 1 |