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A GABA A receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABA A receptor, a ligand-gated ion channel of the major inhibitory neurotransmitter γ-aminobutyric acid (GABA). [1] [2] They are closely related and similar to GABA A receptor antagonists.
First order allosteric modulators: bind to allosteric sites on the receptor complex and affect it either in a positive (PAM), negative (NAM) or neutral/silent (SAM) manner, causing increased or decreased efficiency of the main site and therefore an indirect increase or decrease in Cl − conductance.
The site that an allosteric modulator binds to (i.e., an allosteric site) is not the same one to which an endogenous agonist of the receptor would bind (i.e., an orthosteric site). Modulators and agonists can both be called receptor ligands. [2] Allosteric modulators can be 1 of 3 types either: positive, negative or neutral.
In pharmacology, GABA A receptor positive allosteric modulators, also known as GABAkines or GABA A receptor potentiators, [1] are positive allosteric modulator (PAM) molecules that increase the activity of the GABA A receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system.
Basmisanil (INN Tooltip International Nonproprietary Name; developmental codes RG-1662 and RO5186582) is a highly selective inverse agonist/negative allosteric modulator of α 5 subunit-containing GABA A receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome.
DMCM (methyl 6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate) is a drug from the β-carboline family that induces anxiety and convulsions by acting as a negative allosteric modulator of GABA A receptors — functionally opposite to benzodiazepines and related drugs which are positive allosteric modulators — and is used in scientific research for these properties to test new anxiolytic and ...
About Addex: Addex Therapeutics is a clinical-stage biopharmaceutical company focused on developing a portfolio of novel small molecule allosteric modulators for neurological disorders. Addex lead drug candidate, dipraglurant (mGlu5 negative allosteric modulator or NAM), is under evaluation for future development in brain injury recovery ...
Basmisanil (RG-1662, RO5186582): derivative of Ro4938581, negative allosteric modulator at GABA A α 5, in human trials for treating cognitive deficit in Down syndrome. [ 7 ] L-655,708