Sigma receptors and iboga alkaloids.

摘要: Publisher Summary Current evidence indicates that ibogaine and other iboga alkaloids might produce some of their neurotoxic effects by interaction with sigma-2 receptors. Sigma receptors are membrane proteins bind several psychotropic drugs high affinity. Two major subclasses sigma have been identified. These termed “sigma-1” “sigma-2,” they differentiated pharmacological profile, function, molecular size. Both subtypes to moderate affinity for typical neuroleptics, haloperidol exhibiting the highest both sites. The sigma-1 receptor has cloned in guinea pig, mouse, rat, human, shown be a novel protein > 90% species homology. Some functions attributed include following: (1) modulation synthesis release dopamine acetylcholine, (2) NMDA-type glutamatergic electrophysiology, (3) NMDA-stimulated neurotransmitter release, (4) muscarinic receptor-stimulated phosphoinositide turnover, (5) neuroprotective antiamnesic activity, (6) opioid analgesia, (7) alteration cocaine-induced locomotor activity toxicity. ability ligands induce morphological changes apoptosis led an investigation signaling mechanisms utilized