CP-94,253: a selective serotonin1B (5-HT1B) agonist that promotes satiety

  title={CP-94,253: a selective serotonin1B (5-HT1B) agonist that promotes satiety},
  author={Michelle D. Lee and Kenny J. Simansky},
Abstract The selective 5-HT1B agonist CP-94,253 (3-(1,2,5,6-tetrahydro-4-pyridyl)-5-propoxypyrrolo[3,2-b] pyridine) (5–40 μmol/kg) reduced the intake of both pellets and a 10% solution of sucrose (ID50 = 12.5 and 22.8 μmol/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… 

Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse

5-HT2C-R and 5-HT1B-R activation are each sufficient to induce a hypophagic response, however, concurrent 5- HT2c-R inactivation can potentiate the hypophotic response to 5-ht1b-Ractivation, consistent with an inhibitory role for the 5-hydroxytryptamine-based response in behaviour mediated by the activation of other 4-HT receptors.

Role of 5-HT2C receptors in the hypophagic effect of m-CPP, ORG 37684 and CP-94,253 in the rat

  • R. SchreiberJ. Vry
  • Biology, Medicine
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 2002

Regulation of extracellular concentrations of 5-hydroxytryptamine (5-HT) in mouse striatum by 5-HT(1A) and 5-HT(1B) receptors.

The present findings suggest that, on systemic administration, both 8-OH-PIPAT and CP 94,253 are potent and selective agonists at the somatodendritic 5-HT(1A) autoreceptor and terminal 5- HT(1B/1D) Autoreceptor, respectively, and are each able to cause decreases in extracellular levels in the mouse striatum by activating a distinct set of receptors.



The role of putative 5-HT1A and 5-HT1B receptors in the control of feeding in rats.

The 5-HT1B receptor agonist CP-94,253 reduces food intake and preserves the behavioural satiety sequence

Biochemical and behavioral studies of the 5‐HT1B receptor agonist, CP‐94,253

CP‐94,253, 3‐(1,2,5,6‐tetrahydro‐4‐pyridyl)‐5‐propoxypyrrolo[3,2‐b]pyridine, a new serotonergic ligand, was found to exhibit significantly greater binding affinity at 5‐HT1B receptors than at 5‐HT1A

5-HT1B agonists induce anorexia at a postsynaptic site.

Tolerance to the serotonin 5-HT1 agonist RU 24969 and effects on dopaminergic behaviour.

3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.

2 appears to lie in the ability of a pyrrolo[3,2-b]pyrid-5-one to act as a rotationally restricted bioisosteric replacement for 5-hydroxyindole, which is shown to be biochemically discriminatory in its ability to selectively inhibit forskolin-stimulated adenylate cyclase activity only at the 5-HT1B receptor.

Serotonergic control of the organization of feeding and satiety

  • K. Simansky
  • Biology, Psychology
    Behavioural Brain Research
  • 1995