NBI-27914 (hydrochloride) 是一种选择性 Corticotropin-Releasing Factor 1 (CRF1) 受体拮抗剂，其Ki值 1.7 nM。
| 生物活性 | NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with aKivalue of 1.7 nM[1][3][4]. |
| IC50& Target | Ki: 1.7 nM (CRF1 receptor)[4] |
体内研究
(In Vivo) | NBI 27914 (3~30 mg/kg; i.p.) hydrochloride attenuates the referred abdominal pain at the highest dose tested, it is efficacious both 4 and 24 h post-indomethacin dosing[1].
NBI 27914 (1~10 mg/kg; i.p.) hydrochloride dose dependently attenuates Freund's Complete Adjuvant-induced mechanical hyperalgesia. NBI 27914 (10 mg/kg) hydrochloride reverses the thermal hyperalgesia. NBI 27914 hydrochloride attenuates spinal nerve ligation-induced mechanical hyperalgesia and tactile allodynia with minimal effective doses equal to 5 and 10 mg/kg, respectively[1]. The higher doses of NBI 27914 hydrochloride blocks the behavioral seizures and prevents epileptic discharges in concurrent electroencephalograms recorded from the amygdala[2].
| Animal Model: | Male CD-1 mice (20~25 g)[1] | | Dosage: | 3~30 mg/kg | | Administration: | I.p. | | Result: | Attenuated the referred abdominal pain at the highest dose tested, it was efficacious both 4 and 24 h post-indomethacin dosing. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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