NBI-27914 hydrochloride 

NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a K_i value of 1.7 nM^[1][3][4].

Ki: 1.7 nM (CRF1 receptor)^[4]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

470.65

C₁₈H₂₁Cl₅N₄

1215766-76-9

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [1]. Peng YL, et al. Central Neuropeptide S inhibits food intake in mice through activation of Neuropeptide S receptor. Peptides. 2010;31(12):2259-2263.  [Content Brief]

  [2]. Hummel M, et al. Pain is a salient "stressor" that is mediated by corticotropin-releasing factor-1 receptors. Neuropharmacology. 2010;59(3):160-166.  [Content Brief]

  [3]. Baram TZ, et al. The CRF1 receptor mediates the excitatory actions of corticotropin releasing factor (CRF) in the developing rat brain: in vivo evidence using a novel, selective, non-peptide CRF receptor antagonist. Brain Res. 1997;770(1-2):89-95.  [Content Brief]

  [4]. Chen C, et al. Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists. J Med Chem.  [Content Brief]