LR132 explained

LR132 or (+)-3,4-dichloro-N-[(1R,2S)-2-(1-pyrrolidinyl)cyclohexyl]benzeneethanamine is a selective sigma receptor antagonist, with a reported binding affinity of K_i = 2 ± 0.1 nM for the sigma-1 receptor and more than 350 times selectivity over the sigma-2 receptor.^[1]

Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with LR132 significantly decreases the convulsivity and lethality of cocaine.

See also

• BD1008
• BD1031

Notes and References

1. Matsumoto RR, McCracken KA, Friedman MJ, Pouw B, De Costa BR, Bowen WD . Conformationally restricted analogs of BD1008 and an antisense oligodeoxynucleotide targeting sigma1 receptors produce anti-cocaine effects in mice . Eur. J. Pharmacol. . 419 . 2-3 . 163–74 . 2001 . 11426838. 10.1016/s0014-2999(01)00968-2.