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Description: SHA 68 is a novel, highly potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
References:
1. OkamuraN, et al. Synthesis and pharmacological in vitro and in vivo profile of3-oxo-1, 1-diphenyl-tetrahydro-oxazolo3, 4-apyrazine-7-carboxylic acid4-fluoro-benzylamide (SHA 68), a selective antagonist of theneuropeptide S receptor.J Pharmacol Exp Ther. 2008 Jun; 325(3):893-901.
2. EnshoT, et al. Neuropeptide S increases motor activity and thermogenesis inthe rat through sympathetic activation.Neuropeptides. 2017 Oct; 65:21-27.
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