CP 376395 (CP-316311)

A CRF1 antagonist

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库存: 现货

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5mg

￥1287.00

1030.00

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10mg

￥2100.00

1680.00

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25mg

￥4375.00

3500.00

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50mg

￥8450.00

6760.00

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100mg

￥14825.00

11860.00

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货号: ajce45968
CAS: 175140-00-8
别名: CP 316,311
分子式: C21H30N2O
分子量: 326.48
纯度: >98%
溶解度: DMSO : ≥ 100 mg/mL (306.30 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

CP 376,395 is an antagonist of corticotropin-releasing factor (CRF) receptor 1 (CRF₁; IC₅₀ = 5.1 nM).¹ It inhibits adenylate cyclase activity stimulated by ovine CRF in rat cerebral cortex and at human CRF₁ receptors. CP 376,395 (17.8 mg/kg) inhibits CRF-induced increases in the acoustic startle response in rats. It increases the percentage of open arm entries and time spent in the open arms of the elevated plus maze in mice when administered via intramedial prefrontal cortical injection at doses of 1.5 and 3 nmol.² CP 376,395 (10 mg/kg) reduces ethanol consumption in rats trained on an intermittent access schedule.³ It increases pulmonary ventilation in rats under normocapnic and hypercapnic conditions when injected into the locus coeruleus at a dose of 5 nmol/0.1 μl.⁴

1.Chen, Y.L., Obach, R.S., Braselton, J., et al.2-Aryloxy-4-alkylaminopyridines: Discovery of novel corticotropin-releasing factor 1 antagonistsJ. Med. Chem.51(5)1385-1392(2008) 2.Miguel, T.T., Gomes, K.S., and Nunes-de-Souza, R.L.Tonic modulation of anxiety-like behavior by corticotropin-releasing factor (CRF) type 1 receptor (CRF1) within the medial prefrontal cortex (mPFC) in male mice: Role of protein kinase A (PKA)Horm. Behav.66(2)247-256(2014) 3.Simms, J.A., Nielsen, C.K., Li, R., et al.Intermittent access ethanol consumption dysregulates CRF function in the hypothalamus and is attenuated by the CRF-R1 antagonist, CP-376395Addict. Biol.19(4)606-611(2014) 4.Incheglu, J.M., Bicego, K.C., and Gargaglioni, L.H.Corticotropin-releasing factor in the locus coeruleus as a modulator of ventilation in ratsRespir. Physiol. Neurobiol.23373-80(2016)

Protocol

Animal experiment:

Dogs: Four beagle dogs (two male and two female) weighing between 8 and 15 kg are administered 1 mesylate salt or CP 376395 hydrochloride salt (1.0 mg/kg) into the cephalic vein of the foreleg. The dosing solution for 1 is neat ethanol (15.4 mg/mL) and for CP 376395 is sterile saline at pH 2 (10 mg/mL). Oral dosing is conducted by gavage with drugs suspended in 0.1% methyl cellulose at pH 2. For the intravenous and fasted oral legs of the study, animals have last eaten approximately 21 h prior to drug administration and are permitted food and water approximately 3.5 h postdose. In the fed oral leg of the study, the animals are given one can of wet dog food 1 h before dosing. Blood samples are collected by venipuncture of the jugular vein prior to drug administration and at time points of 0.083 (i.v. only), 0.25, 0.5, 1.0, 2.0, 3.0, 4.0, 6.0, 8.0, 12, and 24 h postdose, processed to obtain serum and stored frozen until the day of analysis[1].

参考文献:

[1]. Chen YL, et al. 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J Med Chem. 2008 Mar 13;51(5):1385-92.