Ibogaine possesses a selective affinity for sigma 2 receptors.
The alkaloid ibogaine is potentially useful to reduce craving for several drugs of abuse, but its mechanism of action is not known. In the current study, in vitro studies were conducted in order to determine the affinity of ibogaine for sigma receptors. Our results indicate that ibogaine has a relatively high affinity for sigma 2 receptors (Ki = 90.4 and 250 nM) and a significantly lower affinity for sigma 1 receptors (Ki = 9310 nM). These data suggest that ibogaine may have a higher affinity at sigma 2 receptors than any other known CNS receptor. Its low affinity for sigma 1 receptors also suggests that ibogaine may be a suitable lead compound for structure-activity relationship studies aimed at developing sigma 2-selective ligands.
Mach
R H
RH
Department of Radiology, Bowman Gray School of Medicine, Wake Forest University, Winston-Salem, NC 27157, USA.
Smith
C R
CR
Childers
S R
SR
D000818:Animals; D006168:Guinea Pigs; D006220:Haloperidol / Q000378:metabolism; D007050:Ibogaine / Q000378:metabolism*; D066298:In Vitro Techniques; D010423:Pentazocine / Q000378:metabolism; D017480:Receptors, sigma / Q000378:metabolism*; D013329:Structure-Activity Relationship
D017480:Receptors, sigma; D007050:Ibogaine; D006220:Haloperidol; D010423:Pentazocine