LR132
 | |
| Systematic (IUPAC) name | |
|---|---|
| (+)-3,4-dichloro-N-[(1R,2S)-2-(1-pyrrolidinyl)cyclohexyl]benzeneethanamine | |
| Clinical data | |
| Identifiers | |
| 135211-15-3 | |
| Chemical data | |
| Formula | C18H26Cl2N2 |
| 341.32 g/mol | |
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 Ki = 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.[1]
See also
References
- ↑ 1.0 1.1 Matsumoto RR, McCracken KA, Friedman MJ, Pouw B, De Costa BR, Bowen WD (2001). "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. doi:10.1016/s0014-2999(01)00968-2.