5 research outputs found
Synthesis, reactivity, and spectral properties of 2,7-difluoro-9-chloromethylenexanthene. Isoelectronicity with heptafulvene derivatives
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On the opioid nature of phencyclidine and its 3-hydroxy derivative
Phencyclidine (PCP) and its 3-hydroxy derivative (PCP-3-OH) caused a dose-dependent, naloxone reversible inhibition of the response of the guinea pig ileum to electrical stimulation. Unlike PCP, PCP-3-OH exerted an opioid antagonistic effect in the mouse vas deferens bioassay. Whereas both compounds displayed a high affinity in displacing [
3H]SKF-10047 binding to rat brain membranes, PCP-3-OH displayed a high affinity to [
3H]morphine receptors also. The mediation of σ- and μ-receptors in the opioid effects of these drugs is discussed
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Receptor binding and antinociceptive properties of phencyclidine opiate-like derivatives
The relative potencies of a new series of phencyclidine (PCP) analogs for the displacement of [3H]morphine binding from rat brain homogenates are well correlated with the relative antinociceptive potencies in the test of writhing induced by acetic acid (0.6%). One group of compoundss exerts a completely naloxone-reversible analgesic effect, while the effects of a second group are only partially reversed by naloxone. These findings and the structural differences between the two groups suggest that their analgesic activity is mediated through different opiate receptors. opiate receptors