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

Solid

Ki: 1.7 nM (CRF1 receptor)

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.
NBI 27914 (1~10 mg/kg; i.p.) hydrochloride dose dependently attenuates Freunds 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. The higher doses of NBI 27914 hydrochloride blocks the behavioral seizures and prevents epileptic discharges in concurrent electroencephalograms recorded from the amygdala.

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

Room temperature or refrigerated transportation.

• [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.  [Information]

  [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.  [Information]

  [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.  [Information]

  [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.  [Information]