Big Bluestem – Andropogon gerardi

by | Dec 10, 2023 | NE Native Grasses

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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. ^ a b 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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