Drug intelligence / Profile preview

tenocyclidine

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

Tenocyclidine is a dissociative anesthetic drug belonging to the arylcyclohexylamine class, structurally related to phencyclidine (PCP) but with a thiophene ring replacing PCP’s benzene ring. It was originally developed by Parke Davis in the late 1950s as an intravenous anesthetic, but clinical development was abandoned due to psychiatric side effects such as emergence delirium. Tenocyclidine acts primarily as a non-competitive antagonist at the N-methyl-D-aspartate (NMDA) receptor, leading to its dissociative and hallucinogenic effects. It also inhibits dopamine reuptake by binding to the dopamine transporter and interacts with other targets including the mu-opioid receptor and α7-subunit of the nicotinic acetylcholine receptor. The drug has been used in research for its high affinity for NMDA receptors and has shown additional pharmacological activities such as antidotal effects against organophosphate poisoning, radioprotective properties, and potential anticancer activity. Tenocyclidine is more potent than PCP and is classified as a Schedule I substance due to its abuse potential[1][2][3][5][6].

Other names
tenociclidina
02

Targets

AcetylcholinesteraseNMDAR (Glutamate receptor ionotropic, NMDA)DAT (Dopamine plasma membrane transport protein)CHRNA7 (α7 nicotinic receptor)MOR (Mu opioid receptor)

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