SHA 68 (i.p.; 5 and 50 mg/kg) reduces NPS-induced horizontal activity and vertical rearing and climbing[1]. SHA 68 (i.v.; 1 mg/kg) has a T1/2 of 0.74 hours, a CL of 4.29 mL/min/kg, and a Vss of 2.53 L/kg[1]. SHA 68 (i.p.; 2.5 mg/kg) has a T1/2 of 0.43 hours, a CL of 4.56 mL/min/kg[1]. Animal Model: Male C57BL/6 mice age 8-12 weeks[1] Dosage: 5 and 50 mg/kg Administration: i.p. Result: Reduced NPS-induced horizontal activity and vertical rearing and climbing. Animal Model: Male C57BL/6 mice age 8-12 weeks[1] Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: i.p. Result: Had a T1/2 of 0.74 hours, a CL of 4.29 mL/min/kg, and a Vss of 2.53 L/kg.
In Vitro
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Okamura N, et al. Synthesis and pharmacological in vitro and in vivo profile of 3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide (SHA 68), a selective antagonist of the neuropeptide S receptor.J Pharmacol Exp Ther. 2008 Jun;325(3):893-901.
[2]. Ensho T, et al. Neuropeptide S increases motor activity and thermogenesis in the rat through sympathetic activation.Neuropeptides. 2017 Oct;65:21-27.
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