ChemInform Abstract: STRUCTURE‐ACTIVITY RELATIONSHIP OF SOME PHENCYCLIDINE DERIVATIVES‐ IN VIVO STUDIES IN MICE

Abstract

Ausgehend von Phencyclidin (I) werden nach angegebenem Schema die Derivate (II)‐(VII) synthetisiert.

Localization of phencyclidine binding sites on alpha and beta subunits of the nicotinic acetylcholine receptor from Torpedo ocellata electric organ using azido phencyclidine

“…The cholinergic effects of PCP and its derivatives have been extensively described Paster et al, 1974;Kloog et al, 1977;Kalir et al, 1978;Petersen and Stillman, 1978). However, it was recognized only recently that these drugs may interact directly with the cholinergic ionophore (Kloog et al, 1979Albuquerque et al, 1980;Oswald and Changeux, 1981a).…”

“…Phencyclidine and 3-aminophencyclidine (l-(1-(3-aminophenyl)-cyclohexyl)piperidine) were prepared as described (Kalir et al, 1978). 3-Azido phencyclidine (l-(1-(3-azidophenyl)-cyclohexyl)piperidine) was prepared from 3-aminophencyclidine by dissolving it in 1 M hydrochloric acid, treating it with KN02, and then adding NaN3 as described previously (Amitai et al, 1982).…”

“…3-Azido phencyclidine (l-(1-(3-azidophenyl)-cyclohexyl)piperidine) was prepared from 3-aminophencyclidine by dissolving it in 1 M hydrochloric acid, treating it with KN02, and then adding NaN3 as described previously (Amitai et al, 1982). Compounds were characterized by C, H, N analysis and infrared spectroscopy and were tested for purity (>98%) by two thin layer chromatography systems (Kalir et al, 1978). The melting point of the AZ-PCP (free base) was 51 to 52°C.…”

“…[3H]PCP (22.5 Ci/mmol) was prepared by catalytic tritium exchange and was tested for purity (>98%) as described elsewhere (Kalir et al, 1978), using a synthetic technique analogous to that described by Kalir et al (1975).…”

“…The existence ' of specific high affinity binding sites of PCP in rat brain tissue has also been demonstrated (Vincent et al, 1979;Zukin and Zukin, 1979). It is not known whether the anticholinergic activity of PCP Paster et al, 1974;Kloog et al, 1977;Kalir et al, 1978) contributes to its psychotic activity. The drug is a potent inhibitor of butyrylcholinesterase Kloog et al, 1977) and can block both muscarinic Kloog et al, 1977) and nicotinic (Kloog et al, 1977;Albuquerque et al, 1980) responses in tissues.…”