Interaction of phencyclidine and its new adamantyl derivatives with muscarinic receptors

Ayala Gabrielevitz; Yoel Kloog; Asher Kalir; David Balderman; Mordechai Sokolovsky

doi:10.1016/0024-3205(80)90051-X

Interaction of phencyclidine and its new adamantyl derivatives with muscarinic receptors

Ayala Gabrielevitz^*, Yoel Kloog, Asher Kalir, David Balderman, Mordechai Sokolovsky

^*Corresponding author for this work

Department of Neurobiology

Tel Aviv University

Research output: Contribution to journal › Article › peer-review

26 Scopus citations

Abstract

The antimuscarinic potency of new derivatives of phencyclidine containing the adamantyl moiety was evaluated in the guinea pig ileum test. The drugs tested competitively inhibited the acetylcholine-induced contractions. K_d values were calculated and compared to those obtained by direct binding to the muscarinic receptors from mouse brain. The new derivative, |1-(2-phenyl-2-adamantyl) piperidine| was found to be the most potent muscarinic antagonist among the many phencyclidine derivatives known to date. The results are discussed in terms of the acetylcholine-like molecular arrangement of these derivatives that gives rise to a characteristic muscarinic interaction.

Original language	English
Pages (from-to)	89-95
Number of pages	7
Journal	Life Sciences
Volume	26
Issue number	2
DOIs	https://doi.org/10.1016/0024-3205(80)90051-X
State	Published - 14 Jan 1980

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abstract = "The antimuscarinic potency of new derivatives of phencyclidine containing the adamantyl moiety was evaluated in the guinea pig ileum test. The drugs tested competitively inhibited the acetylcholine-induced contractions. Kd values were calculated and compared to those obtained by direct binding to the muscarinic receptors from mouse brain. The new derivative, |1-(2-phenyl-2-adamantyl) piperidine| was found to be the most potent muscarinic antagonist among the many phencyclidine derivatives known to date. The results are discussed in terms of the acetylcholine-like molecular arrangement of these derivatives that gives rise to a characteristic muscarinic interaction.",

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AU - Sokolovsky, Mordechai

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N2 - The antimuscarinic potency of new derivatives of phencyclidine containing the adamantyl moiety was evaluated in the guinea pig ileum test. The drugs tested competitively inhibited the acetylcholine-induced contractions. Kd values were calculated and compared to those obtained by direct binding to the muscarinic receptors from mouse brain. The new derivative, |1-(2-phenyl-2-adamantyl) piperidine| was found to be the most potent muscarinic antagonist among the many phencyclidine derivatives known to date. The results are discussed in terms of the acetylcholine-like molecular arrangement of these derivatives that gives rise to a characteristic muscarinic interaction.

AB - The antimuscarinic potency of new derivatives of phencyclidine containing the adamantyl moiety was evaluated in the guinea pig ileum test. The drugs tested competitively inhibited the acetylcholine-induced contractions. Kd values were calculated and compared to those obtained by direct binding to the muscarinic receptors from mouse brain. The new derivative, |1-(2-phenyl-2-adamantyl) piperidine| was found to be the most potent muscarinic antagonist among the many phencyclidine derivatives known to date. The results are discussed in terms of the acetylcholine-like molecular arrangement of these derivatives that gives rise to a characteristic muscarinic interaction.

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Interaction of phencyclidine and its new adamantyl derivatives with muscarinic receptors

Abstract

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