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CGP 71683 hydrochloride
Chemical Name:N-[[trans-4-[[(4-Amino-2-quinazolinyl)amino]methyl]cycl
ohexyl]methyl]-1-naphthalenesulfonamide hydrochloride
Biological Activity:
Extremely selective, non-peptide NPY Y5
receptor antagonist. Displays > 1000-fold selectivity over Y1, Y2
and Y4 receptors; IC50 values are 1.4, 2765, 7187
and 5637 nM at cloned rat Y5, Y1, Y2 and Y4
receptors respectively. Potently inhibits NPY-induced food intake
following i.p. administration in diabetic, free-feeding and fasted rats.
Criscioneet al (1998)
Food intake in free-feeding and energy-deprived lean rats is mediated by the
neuropeptide Y5 receptor. J.Clin.Invest. 102 2136. Dumontet al (2000) Potent and selective tools to investigate neuropeptide Y
receptors in the central and peripheral nervous systems: BIB03304 (Y1) and
CGP71683A (Y5). Can.J.Physiol.Pharmacol. 78 116. Lecklinet
al (2002) Receptor subtypes Y1 and Y5 mediate
neuropeptide Y induced feeding in the guinea-pig. Br.J.Pharmacol. 135
2029.