inverse agonist


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Related to inverse agonist: Partial agonist

inverse agonist

A drug that binds the same cellular receptors as an agonist, but elicits a negative, or opposing cellular response.
See also: agonist
References in periodicals archive ?
Pimavanserin possesses potent 5-HT2A inverse agonist properties required to manage psychosis in PD patients, but lacks clozapine's affinities for [alpha]-1 adrenergic, muscarinic, or histaminergic receptors that contribute to clozapine's poor tolerability.
3) Inverse agonists bind to the same receptor as a normal neurotransmitter or agonist but induce the opposite effect (rather than just preventing neurotransmitter or agonist actions by blocking their interaction with the receptor).
The patent relates to a class of inverse agonists to the 5-HT2A serotonin receptor, which is thought to be involved in the regulation of sleep architecture and sleep maintenance.
The invention also concerns the inverse agonist effect of ML 10375 on 5-HT4(c) and 5-HT4(d) receptors.
Pimavanserin is a 5-HT2A receptor inverse agonist in Phase III development as a treatment for Parkinson's disease psychosis.
Betahistine is an agonist of type 1histamine receptors and an inverse agonist (inhibitor) of type 3 histamine receptor (the negative autoregulatory receptor of histamine), acting in concert to activate the histamine system, which downregulates feeding and enhances alertness and cognition.
Pimavanserin tartrate is a novel, potent and selective 5-HT2A inverse agonist discovered by ACADIA and currently being evaluated in two Phase III pivotal trials as a treatment for PDP.
The data suggest that pimavanserin, a selective serotonin 5-HT2A inverse agonist that does not block dopamine D2 receptors, may provide antipsychotic benefit to patients with PDP without adversely affecting motor function.
In a poster presentation titled "Pimavanserin, a 5-HT2A Receptor Inverse Agonist, Improves Antipsychotic Efficacy and Cognitive Properties of Atypical Antipsychotic Drugs," ACADIA researchers present data showing pimavanserin improves the activity of a number of the most commonly used atypical antipsychotic agents in animal models predictive of antipsychotic efficacy.
Pimavanserin tartrate, previously referred to as ACP-103, is a novel, potent, and selective 5-HT2A inverse agonist that ACADIA discovered and is developing as a treatment for PDP.
ACADIA nominated ACP-106, a proprietary, potent and selective 5-HT2A inverse agonist, as a clinical candidate.
Pimavanserin tartrate (previously referred to as ACP-103) is a novel, potent and selective 5-HT2A inverse agonist that ACADIA discovered and is developing as a co-therapy for schizophrenia and as a treatment for Parkinson's disease psychosis and sleep maintenance insomnia.