LR132

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]

LR132
Identifiers
  • (+)-3,4-dichloro-N-[(1R,2S)-2-(1-pyrrolidinyl)cyclohexyl]benzeneethanamine
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC18H26Cl2N2
Molar mass341.32 g·mol−1
3D model (JSmol)
  • c1cc(c(cc1CCN[C@H]2CCCC[C@H]2N3CCCC3)Cl)Cl
  • InChI=1S/C18H26Cl2N2/c19-15-8-7-14(13-16(15)20)9-10-21-17-5-1-2-6-18(17)22-11-3-4-12-22/h7-8,13,17-18,21H,1-6,9-12H2/t17-,18+/m0/s1
  • Key:NREHOBGKKWFKES-ZWKOTPCHSA-N

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. 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. PMID 11426838.
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