dihydromorphine and 1-(1-phenylcyclohexyl)-4-phenyl-4-piperidinol

dihydromorphine has been researched along with 1-(1-phenylcyclohexyl)-4-phenyl-4-piperidinol* in 2 studies

Other Studies

2 other study(ies) available for dihydromorphine and 1-(1-phenylcyclohexyl)-4-phenyl-4-piperidinol

Article	Year
A novel phencyclidine analog interacts selectively with mu opioid receptors. The Journal of pharmacology and experimental therapeutics, 1984, Volume: 230, Issue:2 A new potent analgesic drug, 1-(1-phenylcyclohexyl)-4-phenyl-4-piperidinol (PCP-4-Ph-4-OH), derived from phencyclidine was tested for its interactions with different types of opioid receptors. The antinociceptive effect of PCP-4-Ph-4-OH in the mouse writhing test (ED50 = 0.3 mg/kg) is reversed by low doses of naloxone (pA2 = 6.98). The potency of PCP-4-Ph-OH in the inhibition of the electrically induced contractions of the guinea-pig ileum (IC50 = 17 nM) is 8-fold higher than that in the mouse vas deferens preparation (IC50 = 130 nM). The concentration of naloxone required to double the IC50 (Ke) of PCP-4-Ph-4-OH is 1.5 to 1.9 nM in both preparations. In opioid radioreceptor assays, PCP-4-Ph-4-OH displays 60- to-300 fold higher affinity for the [3H] dihydromorphine (mu) and D-[3H]Ala2-MePhe-Gly-ol5-enkephalin (mu) binding sites than for D-[3H]Ala2-D-Leu5-enkephalin (delta) sites in rat brain and [3H]bremazocine (kappa) sites in guinea-pig cerebellar membrane preparations. These results suggest that PCP-4-Ph-4-OH interacts with high affinity and selectivity with mu opioid receptors. Topics: Analgesia; Animals; Benzomorphans; Binding, Competitive; Cerebellum; Dihydromorphine; Electric Stimulation; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalin, Leucine; Enkephalin, Leucine-2-Alanine; Enkephalins; Guinea Pigs; Ileum; Male; Mice; Muscle Contraction; Naloxone; Phencyclidine; Rats; Receptors, Opioid; Receptors, Opioid, mu; Vas Deferens	1984
Interaction of two phencyclidine opiate-like derivatives with 3H-opioid binding sites. European journal of pharmacology, 1984, Jun-01, Volume: 101, Issue:3-4 Small modifications of the basic structure of phencyclidine have produced compounds with potent opioid analgesic actions. Detailed competition studies show that two of these phencyclidine derivatives, the 3'-hydroxy and the 4-phenyl-4-hydroxy analogs, displace 3H-opioid binding in a multiphasic manner. Approximately 25% of the total specific binding of all the radiolabeled opioids is displaced by low concentrations of the derivatives while the remainder of the binding is far less sensitive. The inclusion of these derivatives in saturation studies with [3H]dihydromorphine indicate that both compounds interact with highest affinity with mu1 sites. Furthermore, the prior in vivo administration of naloxonazine 24 h earlier reduces the analgesic potency of the 4-phenyl-4-hydroxy compound by 63% supporting a mu1 mechanism of action. Topics: Analgesics; Animals; Binding, Competitive; Dihydromorphine; Male; Naloxone; Phencyclidine; Rats; Rats, Inbred Strains; Receptors, Opioid; Receptors, Opioid, mu	1984

Article

Year

A novel phencyclidine analog interacts selectively with mu opioid receptors.

The Journal of pharmacology and experimental therapeutics, 1984, Volume: 230, Issue:2

A new potent analgesic drug, 1-(1-phenylcyclohexyl)-4-phenyl-4-piperidinol (PCP-4-Ph-4-OH), derived from phencyclidine was tested for its interactions with different types of opioid receptors. The antinociceptive effect of PCP-4-Ph-4-OH in the mouse writhing test (ED50 = 0.3 mg/kg) is reversed by low doses of naloxone (pA2 = 6.98). The potency of PCP-4-Ph-OH in the inhibition of the electrically induced contractions of the guinea-pig ileum (IC50 = 17 nM) is 8-fold higher than that in the mouse vas deferens preparation (IC50 = 130 nM). The concentration of naloxone required to double the IC50 (Ke) of PCP-4-Ph-4-OH is 1.5 to 1.9 nM in both preparations. In opioid radioreceptor assays, PCP-4-Ph-4-OH displays 60- to-300 fold higher affinity for the [3H] dihydromorphine (mu) and D-[3H]Ala2-MePhe-Gly-ol5-enkephalin (mu) binding sites than for D-[3H]Ala2-D-Leu5-enkephalin (delta) sites in rat brain and [3H]bremazocine (kappa) sites in guinea-pig cerebellar membrane preparations. These results suggest that PCP-4-Ph-4-OH interacts with high affinity and selectivity with mu opioid receptors.

Topics: Analgesia; Animals; Benzomorphans; Binding, Competitive; Cerebellum; Dihydromorphine; Electric Stimulation; Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; Enkephalin, Leucine; Enkephalin, Leucine-2-Alanine; Enkephalins; Guinea Pigs; Ileum; Male; Mice; Muscle Contraction; Naloxone; Phencyclidine; Rats; Receptors, Opioid; Receptors, Opioid, mu; Vas Deferens

1984

Interaction of two phencyclidine opiate-like derivatives with 3H-opioid binding sites.

European journal of pharmacology, 1984, Jun-01, Volume: 101, Issue:3-4

Small modifications of the basic structure of phencyclidine have produced compounds with potent opioid analgesic actions. Detailed competition studies show that two of these phencyclidine derivatives, the 3'-hydroxy and the 4-phenyl-4-hydroxy analogs, displace 3H-opioid binding in a multiphasic manner. Approximately 25% of the total specific binding of all the radiolabeled opioids is displaced by low concentrations of the derivatives while the remainder of the binding is far less sensitive. The inclusion of these derivatives in saturation studies with [3H]dihydromorphine indicate that both compounds interact with highest affinity with mu1 sites. Furthermore, the prior in vivo administration of naloxonazine 24 h earlier reduces the analgesic potency of the 4-phenyl-4-hydroxy compound by 63% supporting a mu1 mechanism of action.

Topics: Analgesics; Animals; Binding, Competitive; Dihydromorphine; Male; Naloxone; Phencyclidine; Rats; Rats, Inbred Strains; Receptors, Opioid; Receptors, Opioid, mu

1984