Name | N-[[4-[[(4-aminoquinazolin-2-yl)amino]methyl]cyclohexyl]methyl]naphthalene-1-sulfonamide,hydrochloride |
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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. |
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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 |
Boiling Point | 747.2ºC at 760 mmHg |
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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℃ |