NBI 27914 hydrochloride

Modify Date: 2024-01-12 20:15:01

NBI 27914 hydrochloride Structure
NBI 27914 hydrochloride structure
Common Name NBI 27914 hydrochloride
CAS Number 1215766-76-9 Molecular Weight 470.651
Density N/A Boiling Point N/A
Molecular Formula C18H21Cl5N4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of NBI 27914 hydrochloride


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

 Names

Name 5-Chloro-N-(cyclopropylmethyl)-2-methyl-N-propyl-N'-(2,4,6-trichlorophenyl)-4,6-pyrimidinediamine hydrochloride (1:1)
Synonym More Synonyms

 NBI 27914 hydrochloride Biological Activity

Description NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a Ki value of 1.7 nM[1][3][4].
Related Catalog
Target

Ki: 1.7 nM (CRF1 receptor)[4]

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.
References

[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.

[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.

[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.

[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.

 Chemical & Physical Properties

Molecular Formula C18H21Cl5N4
Molecular Weight 470.651
Exact Mass 468.020874

 Synonyms

4,6-Pyrimidinediamine, 5-chloro-N4-(cyclopropylmethyl)-2-methyl-N4-propyl-N6-(2,4,6-trichlorophenyl)-, hydrochloride (1:1)
5-Chloro-N-(cyclopropylmethyl)-2-methyl-N-propyl-N'-(2,4,6-trichlorophenyl)-4,6-pyrimidinediamine hydrochloride (1:1)
MFCD05662281
5-Chloro-N-(cyclopropylmethyl)-2-methyl-N-propyl-N'-(2,4,6-trichlorophenyl)pyrimidine-4,6-diamine hydrochloride (1:1)
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