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

  title={The anxiolytic‐like effect of 5‐HT1B receptor ligands in rats: a possible mechanism of action},
  author={E. Chojnacka-w{\'o}jcik and Aleksandra Kłodzińska and Ewa Tatarczyńska},
  journal={Journal of Pharmacy and Pharmacology},
We have examined the effect of lesions of 5‐hydroxytryptamine (5‐HT) neurons, produced by p‐chloroamphetamine (p‐CA; 2 times 10 mg kg−1), and the influence of flumazenil (Ro 15–1788, 10 mg kg−1), a benzodiazepine receptor antagonist, on the anxiolytic‐like activity of CP 94253 (5‐propoxy‐3‐(1,2,3,6‐tetrahydro‐4‐pyridinyl)‐1‐H‐pyrrolo[3,2‐b]pyridine), a 5‐HT1B receptor agonist, SB 216641 (N‐[3‐[3‐(dimethylamino)ethoxy]‐4‐methoxyphenyl]‐2′‐methyl‐4′‐(5‐methyl‐1,2,4‐oxadiazol‐3‐yl)‐[1,1′‐biphenyl… 

A and 5 HT 1 B receptors of medial prefrontal cortex modulate anxiogenic-like ehaviors in rats

The role of 5HT1A and5HT1B receptors of the MPFC in modulation of anxiety behaviors in rats was evaluated to evaluate the effects of anxiogenic or anxiolytic drugs in rodents.

Involvement of the 5-HT1A and the 5-HT1B receptor in the regulation of sleep and waking

Overall, most studies support the possibility that stimulation of postsynaptic 5-HT1A receptors, e.g., via systemic administration of a high dose of agonists increases wakefulness and decreases sleep and the mechanism by which 5- HT1B receptors affect state modulation remain elusive.

The 5-HT1B receptor - a potential target for antidepressant treatment

The main focus of this review is the role of 5-HT1BR in relation to MDD and its treatment, although studies of5-HT 1BR in obsessive-compulsive disorder, alcohol dependence, and cocaine dependence are also reviewed.

Dapoxetine Treatment Leads to Attenuation of Chronic Unpredictable Stress Induced Behavioral Deficits in Rats Model of Depression

Investigation of whether repeated administration of dapoxetine at dose 1.0 mg/kg could reversed the behavioral deficits induced by UCMS in rat model of depression foundLocomotive activity in home cage and anxiolytic behavior in light/dark activity box were greater in animals of unstressed group as compared to animals of stressed group.



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

The 5HT1B receptor agonist, CP‐93129, inhibits [3H]‐GABA release from rat globus pallidus slices and reverses akinesia following intrapallidal injection in the reserpine‐treated rat

It is suggested that at least some 5HT1B receptor function as heteroreceptors in the GP, reducing the release of GABA and providing relief of akinesia in the reserpine‐treated rat model of PD.

Serotonin‐1B receptor‐mediated inhibition of [3H]GABA release from rat ventral tegmental area slices

  • Q. YanS. Yan
  • Biology, Chemistry
    Journal of neurochemistry
  • 2001
The hypothesis that 5‐HT1B receptors within the VTA can function as heteroreceptors to inhibit GABA release is supported, suggesting that tritium overflow induced by high potassium derived largely from neuronal stores is explained.

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.

Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig.

Anxiogenic-like effect of serotonin1B receptor stimulation in the rat elevated plus-maze

The role of 5-HT receptor subtypes in the anxiolytic effects of selective serotonin reuptake inhibitors in the rat ultrasonic vocalization test

It is postulate that only 5-HT2A receptors play a pivotal role in the effects of SSRIs in this model of anxiety.

Effects of the non‐NMDA antagonists NBQX and the 2,3‐benzodiazepine GYKI 52466 on different seizure types in mice: comparison with diazepam and interactions with flumazenil

The data indicate that the GABAA receptor‐associated benzodiazepine site is not critically involved in anticonvulsant or adverse effects of GYKI 52466, and demonstrates that non‐NMDA antagonists lack a selective anticonVulsant action in standard models of generalized seizures.

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.