Synthesis and biological activity of phencyclidine and its adamantylamine derivatives

Radioprotective and Antitumor Activity Evaluation of Newly Synthesized Adamantyl Tenocyclidines

“…by the rigid and more liophylic adamantyl moiety showed 2-3-fold enhanced anesthetic effect than PCP. 2 In spite of the numerous published data on the pharmacology of PCP and its adamantyl derivatives, their possible molecular mechanisms of psychomimetic effects is not completely explained. It is known that PCP, TCP, and their adamantyl derivatives (especially TAPIP) act in vivo as open chanel blockers by blocking nicotinic, muscarinic, and N-methyl-D-aspartate (NMDA) receptors.…”

“…Recently we found that adamantyl derivatives of phencyclidine can reduce its toxicity, thus permiting increased dosage. 2 In our previous work we determined the toxicity of PCP and its adamantyl derivatives in mice and cultured cells, and found that all tested adamantyl derivatives were significantly less toxic than PCP. We have also shown that adamantyl derivatives of PCP both in vitro and in vivo exhibit better radioprotective effects than PCP itself.…”

“…We have also shown that adamantyl derivatives of PCP both in vitro and in vivo exhibit better radioprotective effects than PCP itself. 2,3 Investigation of the biological activity of adamantyl derivatives seems to be interesting because of its rather low toxicity and considerable radioprotective and anesthetic effects. This might be even more important considering the fact that the best radioprotectors are sulphurated compounds.…”

Tenocyclidine treatment in soman-poisoned rats--intriguing results on genotoxicity versus protection.

“…Previous studies revealed that both tested compounds exert various pharmacological effects by multiple mechanisms that are not related to AChE interactions (Škare et al, 2002;Ferle-Vidović et al, 1993;1995;Wang et al, 2004a;2004b;Radić et al, 2006). Since both TCP and TAMORF lack the oxime group, it is hard to believe that they can reactivate an already inhibited AChE, like oxime does (Radić et al, 2007).…”

“…These compounds combined with standard therapy effectively antagonize the acute toxicity of soman in mice. According to the preliminary investigations, TCP and its derivatives also possess attractive pharmacological activities such as radioprotective and anticancer effects (Ferle-Vidović et al, 1993;1995;Wang et al, 2004a;2004b).…”