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

Nicole Johnson, Yossef Itzhak, Gavril W. Pasternak

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

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 μ1 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 μ1 mechanism of action.

Original languageEnglish
Pages (from-to)281-284
Number of pages4
JournalEuropean Journal of Pharmacology
Volume101
Issue number3-4
DOIs
StatePublished - Jun 1 1984
Externally publishedYes

Fingerprint

Opiate Alkaloids
Phencyclidine
Opioid Analgesics
Binding Sites
Dihydromorphine
Analgesics

Keywords

  • Opiate receptor μ Site Analgesia Phencyclidine Naloxonazine

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Interaction of two phencyclidine opiate-like derivatives with 3H-opioid binding sites. / Johnson, Nicole; Itzhak, Yossef; Pasternak, Gavril W.

In: European Journal of Pharmacology, Vol. 101, No. 3-4, 01.06.1984, p. 281-284.

Research output: Contribution to journalArticle

Johnson, Nicole ; Itzhak, Yossef ; Pasternak, Gavril W. / Interaction of two phencyclidine opiate-like derivatives with 3H-opioid binding sites. In: European Journal of Pharmacology. 1984 ; Vol. 101, No. 3-4. pp. 281-284.
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