SR 142948 (hydrochloride)

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). It 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 (Cay-20124). It 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.Formal Name: 2-[[[5-(2,6-dimethoxyphenyl)-1-[4-[[[3-(dimethylamino)propyl]methylamino]carbonyl]-2-(1-methylethyl)phenyl]-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid, dihydrochloride. Molecular Formula: C39H51N5O6 . 2HCl. Formula Weight: 758.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 5 mg/ml, PBS (pH 7.2): 0.1 mg/ml. lambdamax: 202, 231 nm. SMILES: CN(CCCN(C)C(C1=CC=C(N2N=C(C(N[C@]3(C(O)=O)[C@H](C4)C[C@H]5C[C@@H]3C[C@@H]4C5)=O)C=C2C6=C(OC)C=CC=C6OC)C(C(C)C)=C1)=O)C.Cl.Cl. InChi Code: InChI=1S/C39H51N5O6.2ClH/c1-23(2)29-21-26(37(46)43(5)15-9-14-42(3)4)12-13-31(29)44-32(35-33(49-6)10-8-11-34(35)50-7)22-30(41-44)36(45)40-39(38(47)48)27-17-24-16-25(19-27)20-28(39)18-24,,/h8,10-13,21-25,27-28H,9,14-20H2,1-7H3,(H,40,45)(H,47,48),2*1H/t24-,25+,27-,28+,39-,,. InChi Key: AQJKZKHTPLUIAD-HAAOKSBBSA-N.