CGP 71683 HYDROCHLORIDE Chemical Properties

storage temp. 

Inert atmosphere,2-8°C

solubility 

H₂O: ~14 mg/mL, soluble

form 

solid

color 

off-white

Safety Information

Safety Statements 

24/25

WGK Germany 

3

CGP 71683 HYDROCHLORIDE Usage And Synthesis

Description

CGP 71683 is an antagonist of neuropeptide Y (NPY) receptor Y₅ (IC₅₀ = 1.4 nM in a radioligand binding assay). It is selective for Y₅ over Y₁, Y₂, and Y₄ receptors (IC₅₀s = 2,765, 7,187, and 5,637 nM, respectively). It inhibits NPY-induced increases in BT-549 cell growth and MDA-MB-231 cell migration when used at a concentration of 0.25 μM. CGP 71683 (10 mg/kg, i.p.) inhibits increases in food intake induced by intracerebroventricular administration of NPY in rats.

Uses

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.

Biological Activity

Extremely selective, non-peptide NPY Y 5 receptor antagonist. Displays > 1000-fold selectivity over Y 1 , Y 2 and Y 4 receptors; IC 50 values are 1.4, 2765, 7187 and 5637 nM at cloned rat Y 5 , Y 1 , Y 2 and Y 4 receptors respectively. Potently inhibits NPY-induced food intake following i.p. administration in diabetic, free-feeding and fasted rats.

in vivo

IC 50

NPY Y₅ receptor

storage

Store at +4°C

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. DOI:10.1038/sj.bjp.0704667
[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. DOI:10.1016/j.regpep.2011.07.001

CGP 71683 HYDROCHLORIDE(192322-50-2)Related Product Information

• CGP 71683 HYDROCHLORIDE
• W-5 HYDROCHLORIDE