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Novel analogues of ketamine and phencyclidine as NMDA receptor antagonists
The identification of structurally novel analogues of ketamine and phencyclidine (PCP), as NMDA receptor antagonists, with low to moderate potency at GluN2A and GluN2B receptors is discussed. In particular, some examples, such as compounds 6 and 10, shows decreased calculated lipophilicity, when compared to PCP, while retaining moderate activity. Moreover, the germinal aryl amino substituted lactam ring, as exemplified in compounds 7-10 and 11-13, constitutes a novel scaffold with potential application in the design of biologically active compounds.
Zarantonello, Paola,Bettini, Ezio,Paio, Alfredo,Simoncelli, Chiara,Terreni, Silvia,Cardullo, Francesco
p. 2059 - 2063
(2011/04/24)

Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site
Two phencyclidine (PCP) analogs, 3 and 4, and one thienylcyclohexylpiperidine (TCP) analog, (±)6, were labeled with positron emitter carbon-11. These compounds displayed higher in vitro binding affinities than PCP itself for the PCP-binding site located inside the ion channel on the N-methyl-D-aspartate (NMDA) receptors. Brain distribution studies in mice showed different uptake characteristics between the PCP and TCP analogs, indicating their different in vivo interactions with the brain components including the PCP-binding site probably due to the different physicochemical properties of the molecules.
Haradahira, Terushi,Sasaki, Sigeki,Maeda, Minoru,Kobayashi, Kaoru,Inoue, Osamu,Tomita, Urara,Nishikawa, Toru,Suzuki, Kazutoshi
p. 843 - 858
(2007/10/03)

Application of chemical P450 model systems to studies on drug metabolism. I. Phencyclidine: A multi-functional model substrate
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Masumoto,Takeuchi,Ohta,Hirobe
p. 1788 - 1794
(2007/10/02)