Direclidine

Direclidine (i.e., NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor. It has no specified IC50/EC50/Ki values, is orally effective, and there is no clear literature mentioning whether it crosses the blood-brain barrier. It has extremely low affinity for M1, M2, M3, and M5 receptors and binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Its mechanism of action involves specifically activating 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. Detailed in vitro/in vivo data on the key active ingredient have not yet been publicly disclosed (only the completion of Phase I clinical trials has been mentioned, but the results have not been published). Its core function is to improve symptoms associated with neuropsychiatric disorders, and its main research area is the treatment of schizophrenia and other neuropsychiatric disorders. It has no natural source and is an artificially designed and synthesized small molecule compound^[1].

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