SR 142948A

SR 142948A用途

IC50为1.19 nM的强效,选择性和口服活性神经降压素受体拮抗剂；拮抗HT 29细胞中神经降压素诱导的肌醇一磷酸形成,IC50为3.9 nM,抑制神经降压素诱导的小鼠转向行为,以0.1mg/kg完全拮抗大鼠纹状体中神经降压素诱发的乙酰胆碱释放；还阻断通过静脉内注射神经降压素注射到腹侧被盖区域诱导的低温和镇痛。

SR 142948A名称

[ CAS 号 ]:
184162-21-8

[ 中文名 ]:
SR 142948A

[ 英文名 ]:
SR 142948A

[英文别名 ]:

MFCD03106502
SR 142948 hydrochloride
SR 142948A

SR 142948A生物活性

[ 描述 ]:

[参考文献]

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

SR 142948A物理化学性质

[ 分子式 ]:
C₃₉H₅₁N₅O₆

[ 分子量 ]:
722.313

[ 精确质量 ]:
721.360596

[ 外观性状 ]:
固体

[ 储存条件 ]:
2-8°C

SR 142948A安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

SR 142948A文献

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) ...

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