Direclidine (NBI-1117568, HTL-0016878) citrate is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. Direclidine citrate binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine citrate specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine citrate can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders [1].
In Vitro, Direclidine citrate is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. Direclidine citrate binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine citrate specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine citrate can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders[1].
References:
[1]. Palma JA. Muscarinic control of cardiovascular function in humans: a review of current clinical evidence. Clinical autonomic research: official journal of the Clinical Autonomic Research Society. 2024 Feb;34(1):31-44.
In Vitro, Direclidine citrate is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. Direclidine citrate binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine citrate specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine citrate can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders[1].
References:
[1]. Palma JA. Muscarinic control of cardiovascular function in humans: a review of current clinical evidence. Clinical autonomic research: official journal of the Clinical Autonomic Research Society. 2024 Feb;34(1):31-44.