A neuropeptide with diverse biological activities
货号:ajcx23516
CAS:N/A
分子式:C39H51N5O6.2HCl
分子量：758.8
溶解度:DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 0.1 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SR 142948 is an orally bioavailable non-peptide antagonist of neurotensin receptors (NTS; IC₅₀s = 1.19, 0.32, and 3.96 nM for human recombinant NTS receptors expressed in CHO cells, HT-29 cells, and adult rat brain membranes, respectively).¹It inhibits inositol phosphate formation in HT-29 cells (IC₅₀= 3.9 nM) and intracellular calcium accumulation in CHO cells expressing human NTS receptors. SR 142948 (1 mg/kg, i.v.) inhibits the firing rate of rat ventral pallidum neurons with a longer duration of action than the NTS receptor antagonist SR 48692 .²It also inhibits neurotensin-induced behavioral responses, including inhibition of neurotensin-induced turning behavior in mice when administered at doses ranging from 40 to 640 mg/kg and hypothermia and analgesia in rats and mice.¹

1.Gully, D., Labeeuw, B., Boigegrain, R., et al.Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonistJ. Pharmacol. Exp. Ther.280(2)802-812(1997) 2.Michaud, J.-C., Gueudet, C., and SoubriÉ, P.Effects of neurotensin receptor antagonists on the firing rate of rat ventral pallidum neuronsNeuroreport11(7)1437-1441(2000)