Lee M D, Simansky K J
Department of Pharmacology, Hahnemann School of Medicine, Allegheny University of the Health Sciences, Philadelphia, PA 19129, USA.
Psychopharmacology (Berl). 1997 Jun;131(3):264-70. doi: 10.1007/s002130050292.
The selective 5-HT1B agonist CP-94,253 (3- (1,2,5,6-tetrahydro-4-pyridyl)-5-propoxypyrrolo[3, 2-b] pyridine) (5-40 mumol/kg) reduced the intake of both pellets and a 10% solution of sucrose (ID50 = 12.5 and 22.8 mumol/kg, respectively) in mildly deprived rats. Time-sampled observations revealed that CP-94,253 terminated feeding earlier, without disrupting the continuity of feeding. CP-94,253 increased standing but did not promote resting during satiation. Microstructural analysis of licking indicated that CP-94,253 decreased the frequency, but not the size, of bursts and clusters of licks without altering oral motor efficiency. The peripherally acting 5-HT1B agonist, CP-93,129 (3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one) had no effect on food intake. These results imply that CP-94,253 probes a role for central 5-HT1B receptors in the regulation of meal size and duration, but that recruitment of other 5-HT receptor subtypes may be needed for the full expression of satiety.
选择性5-羟色胺1B（5-HT1B）激动剂CP-94,253（3-(1,2,5,6-四氢-4-吡啶基)-5-丙氧基吡咯并[3,2-b]吡啶）（5-40微摩尔/千克）可减少轻度饥饿大鼠的颗粒饲料和10%蔗糖溶液的摄入量（半数抑制剂量分别为12.5和22.8微摩尔/千克）。定时取样观察显示，CP-94,253能提前终止进食，且不干扰进食的连续性。CP-94,253会增加大鼠站立次数，但在饱腹感期间不会促进其休息。舔舐的微观结构分析表明，CP-94,253降低了舔舐爆发和集群的频率，但不改变其大小，且不影响口腔运动效率。外周作用的5-HT1B激动剂CP-93,129（3-(1,2,5,6-四氢吡啶-4-基)吡咯并[3,2-b]吡啶-5-酮）对食物摄入量没有影响。这些结果表明，CP-94,253揭示了中枢5-HT1B受体在调节进餐量和进餐持续时间方面的作用，但可能需要募集其他5-HT受体亚型才能充分发挥饱腹感。
