SR 142948A

Names

[ Name ]:
SR 142948A

[Synonym ]:
MFCD03106502
SR 142948 hydrochloride
(1R,5R)-2-({[5-(2,6-Dimethoxyphenyl)-1-(4-{[3-(dimethylamino)propyl](methyl)carbamoyl}-2-isopropylphenyl)-1H-pyrazol-3-yl]carbonyl}amino)-2-adamantanecarboxylic acid hydrochloride (1:1)
2-[[5-(2,6-dimethoxyphenyl)-1-(4-(N-(3-dimethylaminopropyl)-N-methylcarbamoyl)-2-isopropylphenyl)-1H-pyrazole3-carbonyl]amino] adamantane-2-carboxylic acid hydrochloride
SR 142948A
Tricyclo[3.3.1.13,7]decane-2-carboxylic acid, 2-[[[5-(2,6-dimethoxyphenyl)-1-[4-[[[3-(dimethylamino)propyl]methylamino]carbonyl]-2-(1-methylethyl)phenyl]-1H-pyrazol-3-yl]carbonyl]amino]-, (1R,5R)-, hydrochloride (1:1)

Biological Activity

[Description]:

A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM; antagonizes neurotensin-induced inositol monophosphate formation in HT 29 cells with IC50 of 3.9 nM, inhibits the turning behavior induced by neurotensin in mice, completely antagonizes neurotensin-evoked acetylcholine release in the rat striatum at 0.1 mg/kg; also blocks both hypothermia and analgesia induced by i.c.v. injection of neurotensin injection into the ventral tegmental area.

[References]

References 1. Gully D, et al. J Pharmacol Exp Ther. 1997 Feb;280(2):802-12. 2. Betancur C, et al. Eur J Pharmacol. 1998 Feb 5;343(1):67-77. 3. Schaeffer P, et al. J Cardiovasc Pharmacol. 1998 Apr;31(4):545-50. View Related Products by Target Neurotensin Receptor

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₉H₅₁N₅O₆

[ Molecular Weight ]:
722.313

[ Exact Mass ]:
721.360596

[ Storage condition ]:
2-8°C

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.

J. Pharmacol. Exp. Ther. 280(2) , 802-12, (1997)

SR 142948A, 2-[[5-(2,6-dimethoxyphenyl)-1-(4-(N-(3-dimethylaminopropyl)-N-methylc arbamoyl)-2-isopropylphenyl)-1H-pyrazole3-carbonyl]amino] adamantane-2-carboxylic acid, hydrochloride, a new and extre...

Neurotensin receptor antagonist SR 142948A alters Fos expression and extrapyramidal side effect profile of typical and atypical antipsychotic drugs.

Biol. Psychiatry 29(12) , 2200-7, (2004)

Antipsychotic drugs (APDs) have previously been shown to alter Fos expression in a regionally specific manner. Increases in Fos expression in the nucleus accumbens (NAcc) are common to all clinically ...

Neurotensin signaling induces intracellular alkalinization and interleukin-8 expression in human pancreatic cancer cells.

Mol. Oncol. 3(3) , 204-13, (2009)

Pancreatic adenocarcinomas express neurotensin receptors in up to 90% of cases, however, their role in tumor biology and as a drug target is not clear. In the present study, a stable neurotensin (NT) ...