The company's lead product is an alpha-7 nicotinic acetylcholine receptor
agonist and has been tested in Phase IIa clinical trials for cognition disorders in Alzheimer's disease and schizophrenia.
Selective changes in nicotinic acetylcholine receptor
subtypes related to tobacco smoking: an immuno-histochemical study.
Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor
partial agonist, vs.
Solubilization and hydrodynamic properties of pig atrial muscarinic acetylcholine receptor
Molecular blueprint of novel allosteric binding sites in the agonist-binding domain of the ui7 nicotinic acetylcholine receptor
, PNAS, 2015, 112(19):E2543-E2552 (DOI:10.
Whether the molecule in its current form binds too many types of acetylcholine receptors
, whether it activates other neurological systems or whether suicide risk is simply elevated among people giving up cigarettes is unknown.
Bionomics' lead drug candidate BNC210, currently in Phase 2 for the treatment of generalized anxiety disorder, is a novel, proprietary negative allosteric modulator of the alpha-7 nicotinic acetylcholine receptor
Karuna's lead program, KarXT, is a product candidate consisting of xanomeline, a novel clinical-stage muscarinic acetylcholine receptor
agonist (activator) that has demonstrated efficacy in reducing psychosis and improving cognition in placebo-controlled human trials, and trospium chloride, an FDA-approved and well-established muscarinic receptor antagonist (blocker) that studies have shown does not enter the central nervous system.
This type of acetylcholine receptor
consists of multiple protein subunits, which form an ion channel in the cell membrane, and, as the name implies, also binds to nicotine.
Varenicline is a [alpha]4[beta]2 nicotinic acetylcholine receptor
partial agonist which is used for the cessation of smoking (4).
NEUROIMMUNOLOGY ACETYLCHOLINE RECEPTOR
AUTOANTIBODY (ACHRAB) KITS--BINDING AND BLOCKING
Bupropion is also a nicotinic acetylcholine receptor
inhibitor and used for smoking cessation.