Carbetapentane

Carbetapentane is a non-opiod small molecule agonist of sigma sites, producing antitussive and anticonvulsant effects. Carbetapentane is described to protect rats against maximal electroshock-induced seizures. A study demonstrates that the attenuation of kainic acid-induced neurotoxicity by Carbetapentane is overriden by a sigma-1 receptor antagonist, indicating that Carbetapentane produces neuroprotection through its sigma site binding activity. Binding activity on muscarinic receptors is also reported, though Carbetapentane did not provide protection against NMDA lethality and therefore does not demonstrate the NMDA-antagonist action ascribed to the closely related antitussive and anticonvulsant Dextromethorphan. Carbetapentane is an inhibitor of KOR-3 and an activator of Sigma Receptor.