inverse agonist

(redirected from Inverse agonists)

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 ?
The article was written by an independent Japanese research group and presents the outcomes of a study on the role of histamine in the recollection of forgotten memories and the effects of using histamine H3 receptor inverse agonists for treatment.
The granted claims of the patents include the class of selective H3 Inverse agonists and 5HT6 compounds respectively and are being developed as therapeutic agents for major depressive disorders and for the treatment of cognitive impairment associated with neurodegenerative disorders like Alzheimer's disease, Attention deficient hyperactivity disorder (ADHD), Huntington's disease, Narcolepsy, Parkinson and Schizophrenia respectively.
SMLs that might be developed for the treatment of GD are SML TSHR antagonists and SML TSHR inverse agonists.
New in vitro tools to study human constitutive androstane receptor (CAR) biology: discovery and comparison of human CA inverse Agonists. Mol.
These findings are in agreement with the current view that [CysLT.sub.1] inverse agonists decrease seizures (10,11), and extend from previous data showing that systemic montelukast impairs kindling induction with PTZ (9).
On the cellular surface, both active and inactive [H.sub.1]-receptors exist in equilibrium, responding to histamines (agonists) and inverse agonists (antihistamines).
This basal activity can be suppressed by odorants functioning as inverse agonists.
For example, GABAA receptor antagonists and inverse agonists (3) decrease alcohol self-administration in animals (Hyytia and Koob 1995; Rassnick et al.
Biochemists and other scientists synthesize the current understanding of such aspects as structure-activity relationships and conformational freedom of CB1 receptor antagonists and inverse agonists, cannabinoid receptor signal transduction pathways, mutational analyses of the receptors, new insights into the endo-cannabinoid system using knockout mice, and therapeutic applications for agents that act at CB1 and CB2 receptors.
In some embodiments the altered versions of CXCR3 are used, inter alia, for the direct identification of candidate compounds such as receptor agonists, inverse agonists, partial agonist or antagonist for use in, for example and not limitation, graft rejection; inflammatory skin disease; inflammatory bowel disease; allergic inflammation, allergic pulmonary inflammation, inflammatory demyelinating neuropathy, CNS inflammation; rheumatoid arthritis, bronchiolitis obliterans syndrome, periodontal disease and neurodegenerative disease.
First, the benzodiazepine inverse agonists methyl 6,7-dimethoxy-4-ethyl-[Beta]-carboline-3-carboxylate (DMCM) and n-butyl-[Beta]-carboline-3-carboxylate (CCB) enhanced the GABA-mediated responses; second, at low concentrations, zinc produced a similar enhancement of the responses to GABA.
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.