European journal of pharmacology
June 6, 1995
W D Bowen, B J Vilner, W Williams et al.
95 citations
Ibogaine binds moderately to sigma-2 receptors (Ki = 201 nM) and weakly to sigma-1 receptors (Ki = 8554 nM), showing 43-fold selectivity for sigma-2. Related compounds tabernanthine and ibogamine also bind sigma-2 with similar affinity but have higher sigma-1 affinity, resulting in about 14-fold selectivity. A potential ibogaine metabolite, O-des-methyl-ibogaine, has much weaker sigma-2 affinity (Ki = 5226 nM) and no significant sigma-1 affinity. Coronaridine and harmaline lack significant affinity for either sigma subtype. These findings suggest sigma-2 receptors may contribute to ibogaine's effects.
Synapse (New York, N.Y.)
August 1, 1991
H C Akunne, A A Reid, A Thurkauf et al.
The brain contains two types of PCP binding sites: site 1 (linked to the NMDA receptor) and site 2 (linked to the dopamine reuptake complex). This work examined brain membranes from multiple species and found detectable site 2 in guinea pig, rabbit, pig, mouse, sheep, and human, but not in rat or chicken. In human cortex, site 2 was the predominant binding site. Dopamine and serotonin uptake inhibitors produced a wash-resistant inhibition of [3H]TCP binding to site 2 but not site 1. The results suggest human cortex possesses high-affinity PCP binding sites associated with biogenic reuptake binding sites, and that guinea pig, but not rat, may be an appropriate animal model for studying PCP site 2 in human brain.
Neuropharmacology
September 1, 1990
A A Reid, M V Mattson, B R De Costa et al.
Phencyclidine (PCP) and its analog TCP bind non-selectively to two high-affinity binding sites in guinea pig brain: one coupled to the NMDA glutamate receptor (site 1) and the other associated with the dopamine reuptake carrier (site 2). The compound (+)MK801 is highly selective for site 1 and produces minimal psychotomimetic effects in humans at doses that reduce seizures, whereas PCP produces psychotomimetic effects. This suggests that (+)MK801 can serve as a marker for site 1 and that PCP's psychotomimetic effects may be mediated by site 2.