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192322-50-2

192322-50-2 structure
192322-50-2 structure
  • Name: CGP 71683 HCl
  • Chemical Name: N-[[4-[[(4-aminoquinazolin-2-yl)amino]methyl]cyclohexyl]methyl]naphthalene-1-sulfonamide,hydrochloride
  • CAS Number: 192322-50-2
  • Molecular Formula: C26H30ClN5O2S
  • Molecular Weight: 512.06700
  • Catalog: Signaling Pathways GPCR/G Protein Neuropeptide Y Receptor
  • Create Date: 2017-06-26 01:43:21
  • Modify Date: 2024-01-12 11:34:50
  • CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.

Name N-[[4-[[(4-aminoquinazolin-2-yl)amino]methyl]cyclohexyl]methyl]naphthalene-1-sulfonamide,hydrochloride
Synonyms UNII-45B73P82A3
GNF-Pf-1864
CGP-71683A
Description CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.
Related Catalog
Target

Ki: 1.3 nM (Y5 receptor), 200 nM (Y2 receptor), >4000 nM (Y1 receptor)[1]

In Vitro CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes[1].
In Vivo CGP71683 (15 nmol/rat, icv, twice daily) shows anorexigenic effect, reducing food intake and bady weight of fed rats. CGP71683 causes 3-times higher serum total T4 and 37% increase in free T4 in the fasted rats than in the fasted controls rats[2].
Animal Admin Rats[2] CGP71683 is dissolved in 30% DMSO and kept frozen at -20°C until the experiment. Each microinjection consists of 2 μL of either vehicle (30% DMSO) or CGP71683 (7.5 nmol/μL; 15 nmol/rat) injected during 30-60 s through the guide cannula, as the following protocols: I - rats with free access to chow receive 6 microinjections (15 nmol/rat, 10-14 h interval between each one) and are killed 1 h after the last injection, between 9 and 10 a.m. Food intake is estimated by the reduction in chow mass (g), evaluated daily, immediately before each icv injection. II - 72 h-fasted rats receive a single microinjection of vehicle or CGP71683 (15 nmol/rat) and sacrificed 1 h latter. III - during a period of 72 h of fasting, rats are treated with multiple injections of vehicle or CGP71683 with the same protocol used for fed animals, and the fasting period started 10 h before the first microinjection. At the end of experimental protocols, rats are decapitated and serum is obtained from trunk blood for the measurement of the concentrations of hormones[2].
References

[1]. Lecklin A, et al. Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Br J Pharmacol. 2002 Apr;135(8):2029-37.

[2]. Costa-e-Sousa RH, et al. Central NPY-Y5 receptors activation plays a major role in fasting-induced pituitary-thyroid axis suppression in adult rat. Regul Pept. 2011 Nov 10;171(1-3):43-7.

Boiling Point 747.2ºC at 760 mmHg
Molecular Formula C26H30ClN5O2S
Molecular Weight 512.06700
Flash Point 405.7ºC
Exact Mass 511.18100
PSA 118.38000
LogP 7.48990
Vapour Pressure 1.19E-22mmHg at 25°C
Storage condition 2-8℃
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