CP-135,807, a selective 5-HT1D agonist: effects in drug discrimination and punishment procedures in the pigeon

  title={CP-135,807, a selective 5-HT1D agonist: effects in drug discrimination and punishment procedures in the pigeon},
  author={Robert S. Mansbach and Charles C. Rovetti and John Eugene Macor},
Abstract CP-135,807 [3-(N-methylpyrrolidin-2R-ylmeth- yl)-5-(3-nitropyrid-2-yl)amino-1H-indole] binds with high affinity to central 5-HT1D receptors, and in functional studies produces dose-dependent decreases in extracellular serotonin. These and other findings have suggested that CP-135,807 may act as a terminal 5-HT autoreceptor agonist. In an attempt to characterize the behavioral activity of selective 5-HT1D ligands, adult male Carneau pigeons were trained to discriminate IM injections of… 

Behavioral Pharmacology of AR-A000002, a Novel, Selective 5-Hydroxytryptamine1B Antagonist

Data suggest utility for 5-HT1B antagonists in the treatment of both anxiety and affective disorders.

Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression

The results indicate that the selective agonist (CP 94253) and antagonists (SB 216641 and GR 127935) of 5-HT1B receptors produce effects that are characteristic of anxiolytics, in the preclinical models used; however, CP 94253 also behaves like an antidepressant drug.

The discriminative stimulus properties of LY233708, a selective serotonin reuptake inhibitor, in the pigeon

It is demonstrated that an SSRI can induce a specific, stable discriminative stimulus that appears to involve activation of the 5-HT1A receptor in the pigeon.

The anxiolytic‐like effect of 5‐HT1B receptor ligands in rats: a possible mechanism of action

The results suggested that the anxiolytic‐like effect of the 5‐HT1B receptor ligands CP 94253, SB 216641 and GR 127935 was possibly linked to the postsynaptic 5‐ht1B receptors or/and 5‐ HT1B heteroreceptors.

Cannabinoids and drugs of abuse



Studies on the neuronal circuits involved in the discriminative stimulus effects of 5-hydroxytryptamine1A receptor agonists in the rat.

The results suggest that the discriminative stimulus properties of both 8-OH-DPAT and 5-OMe-DMT are 5-HT1A receptor mediated, although 5-Omethoxy-N,N-dimethyltryptamine may involve an additional interaction with other 5- HT receptor subtypes.

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

Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes

  • R. E. HeuringS. Peroutka
  • Biology, Chemistry
    The Journal of neuroscience : the official journal of the Society for Neuroscience
  • 1987
The data demonstrate the presence of a homogeneous class of 5- HT1 binding sites in bovine caudate that is pharmacologically distinct from previously defined 5-HT1A, 5-ht1B, 5 - HT1C, 4-HT2, 3-HT3 receptor subtypes.

Imipramine as a discriminative stimulus.

  • L. ZhangJ. Barrett
  • Psychology, Biology
    The Journal of pharmacology and experimental therapeutics
  • 1991
This appears to be the first report of the successful, long-term establishment of imipramine as a discriminative stimulus without the development of toxicity and confirms reports that compounds active at this receptor site may have antidepressant activity.

Behavioral studies with anxiolytic drugs. III. Antipunishment actions of buspirone in the pigeon do not involve benzodiazepine receptor mechanisms.

Findings confirm previous work demonstrating marked rate-increasing effects of buspirone on punished responding in the pigeon, extend such effects to the busPirone analog MJ 13805 and indicate that the effects ofBuspirone are not mediated through the benzodiazepine receptor complex.

Discriminative stimulus properties of buspirone in the pigeon.

These findings support recent behavioral and receptor binding studies suggesting that serotonin receptors, and 5-hydroxytryptamine-1A receptors in particular, may be responsible for mediating the anticonflict effects of buspirone and other atypical anxiolytics.