CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity

  title={CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity},
  author={Judith A. Siuciak and Douglas S. Chapin and Sheryl A. McCarthy and Victor Guanowsky and Janice A. Brown and Phoebe Chiang and Ravi B. Marala and Terrell Ann Patterson and Patricia A. Seymour and Andrew G. Swick and Philip A. Iredale},

S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models

In vitro and in vivo, the novel benzourea derivative, S32006 is a potent 5-HT2C receptor antagonist, and possesses antidepressant and anxiolytic properties in diverse rodent models.

5-HT2C Agonists Modulate Schizophrenia-Like Behaviors in Mice

These results provide additional evidence that 5-HT2C receptors are suitable drug targets with fewer side effects, greater therapeutic selectivity, and enhanced efficacy for treating schizophrenia and related disorders than current APDs.

Evaluation of chemically diverse 5-HT2C receptor agonists on behaviours motivated by food and nicotine and on side effect profiles

These studies support the utility of 5-HT2C agonists as a therapeutic approach to treat nicotine dependence and plasma exposure levels after acute lorcaserin treatment suggest that equivalent dosages could be used to evaluate these drugs in obesity and smoking cessation trials.

Effects of ST2472, a novel antipsychotic, on prepulse inhibition.

A Novel Aminotetralin-Type Serotonin (5-HT) 2C Receptor-Specific Agonist and 5-HT2A Competitive Antagonist/5-HT2B Inverse Agonist with Preclinical Efficacy for Psychoses

Results indicate a 5-HT2C receptor-specific agonist, such as (−)-MBP, may be pharmacotherapeutic for psychoses, without liability for obesity, hallucinations, heart disease, sedation, or motoric disorders.

Repeated administration of 5‐hydroxytryptamine 2C agonist MK212 produces a sensitization effect of antipsychotic activity

Results from this study suggest that repeated treatment of MK212 is capable of inducing a dose‐dependent sensitization of antipsychotic activity in conditioned avoidance response and MK801‐induced hyperlocomotion tests.

The role of serotonin in the NMDA receptor antagonist models of psychosis and cognitive impairment

Multiple 5-HT receptors contribute to effective treatments to reverse adverse effects of NMDA-RA which model psychosis and cognitive impairment, suggesting the importance of the constitutive activity of 5- HT2C receptors in NOR.

5-HT(2C) agonists as therapeutics for the treatment of schizophrenia.

The preclinical profile of 5-HT(2C) agonists from a neurochemical, electrophysiological, and a behavioral perspective is indicative of antipsychotic-like efficacy without extrapyramidal symptoms or weight gain.

Evaluation of Selective 5-HT2C Agonists in Acute Seizure Models.

Overall, at doses known to interact with 5-HT2CR, there was no clear class-related effect of these agonists in any test, and the only notable antiseizure effect of fenfluramine was inhibition of MES-induced tonic seizures in the rat.



Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies.

The data indicate that MDL 100,907 has a clozapine-like profile of potential antipsychotic activity with low extrapyramidal sid-effect liability.

Antidepressant-like behavioral effects mediated by 5-Hydroxytryptamine(2C) receptors.

  • J. CryanI. Lucki
  • Biology, Psychology
    The Journal of pharmacology and experimental therapeutics
  • 2000
The results strongly implicate a role for 5-HT(2C) receptors in the behavioral effects of antidepressant drugs and exemplify the benefits of using the modified rat forced swim test, which was sensitive to serotonergic compounds and distinguished behavioral changes associated with serotoneric and noradrenergic effects.

m-Chlorophenylpiperazine (mCPP) is an antagonist at the cloned human 5-HT2B receptor.

This study suggests that any 5-HT2B receptor-mediated effects are more likely to result from receptor blockade than from receptor activation, and supports the proposal that at least some of the clinical effects of mCPP are likely to be mediated via stimulation of the 5- HT2C receptor.

The 5-HT2A receptor antagonist M100907 is more effective in counteracting NMDA antagonist- than dopamine agonist-induced hyperactivity in mice

It is drawn that a 5-HT2A receptor antagonist, due to i a the low side effect liability, could be the preferable treatment strategy in various disorders associated with hypoglutamatergia; such conditions might include schizophrenia, childhood autism and dementia disorders.