WRYamide，一种基于神经肽Y的三肽，可拮抗大鼠的进食行为。

WRYamide, a NPY-based tripeptide that antagonizes feeding in rats.

作者信息

Chance W T, Tao Z, Sheriff S, Balasubramaniam A

机构信息

Department of Surgery, University of Cincinnati Medical Center, 231 Bethesda Avenue, Cincinnati, OH 45267, USA.

出版信息

Brain Res. 1998 Aug 24;803(1-2):39-43. doi: 10.1016/s0006-8993(98)00574-5.

DOI:10.1016/s0006-8993(98)00574-5

PMID:9729264

Abstract

Modifications of (D-Trp32) neuropeptide Y (NPY) led to the development of potential peptide-based lower molecular weight (500-800 Da) NPY feeding antagonists. One compound, WRYamide (N-Ac-Trp-Arg-Tyr-NH2), blocked NPY-induced feeding for 1 to 4 h when injected intrahypothalamically (i.h.t.) at 1 to 40 microgram. Schedule-induced feeding was also antagonized for up to 24 h by 20 microgram of WRYamide, i.h.t. Injection of 2.5 mg/kg (1 mg/rat) of WRYamide, i.v., also reduced significantly schedule-induced feeding for 4 h. A conditioned taste aversion could not be classically conditioned to saccharin using WRYamide as the unconditioned stimulus. These results may lead to the development of systemically active anti-obesity drugs.

摘要

（D-色氨酸32）神经肽Y（NPY）的修饰导致了潜在的基于肽的低分子量（500-800道尔顿）NPY摄食拮抗剂的开发。一种化合物，WRY酰胺（N-乙酰基-色氨酸-精氨酸-酪氨酸-NH2），当以1至40微克的剂量下丘脑内注射（i.h.t.）时，可阻断NPY诱导的摄食1至4小时。20微克的WRY酰胺，i.h.t.，也可使定时诱导摄食拮抗长达24小时。静脉注射2.5毫克/千克（1毫克/大鼠）的WRY酰胺也可显著减少定时诱导摄食4小时。使用WRY酰胺作为非条件刺激物，不能使对糖精的条件性味觉厌恶经典性条件化。这些结果可能会导致开发出具有全身活性的抗肥胖药物。