Moehle, Mark S.; Bender, Aaron M.; Dickerson, Jonathan W.; Foster, Daniel J.; Qi, Aidong; Cho, Hyekyung P.; Donsante, Yuping; Peng, Weimin; Bryant, Zoey; Stillwell, Kaylee J.; Bridges, Thomas M.; Chang, Sichen; Watson, Katherine J.; O’Neill, Jordan C.; Engers, Julie L.; Peng, Li; Rodriguez, Alice L.; Niswender, Colleen M.; Lindsley, Craig W.; Hess, Ellen J.; Conn, P. Jeffrey; Rook, Jerri M. published the article 《Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy》. Keywords: muscarinic acetylcholine receptor antagonist antiparkinson antidystonic Parkinson disease.They researched the compound: 4,4-Difluoropiperidine hydrochloride( cas:144230-52-4 ).COA of Formula: C5H10ClF2N. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:144230-52-4) here.
Nonselective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some movement disorders, including Parkinson’s disease and dystonia. Despite their efficacy in these and other central nervous system disorders, antimuscarinic therapy has limited utility due to severe adverse effects that often limit their tolerability by patients. Recent advances in understanding the roles that each mAChR subtype plays in disease pathol. suggest that highly selective ligands for individual subtypes may underlie the antiparkinsonian and antidystonic efficacy observed with the use of nonselective antimuscarinic therapeutics. Our recent work has indicated that the M4 muscarinic acetylcholine receptor has several important roles in opposing aberrant neurotransmitter release, intracellular signaling pathways, and brain circuits associated with movement disorders. This raises the possibility that selective antagonists of M4 may recapitulate the efficacy of nonselective antimuscarinic therapeutics and may decrease or eliminate the adverse effects associated with these drugs. However, this has not been directly tested due to lack of selective antagonists of M4. Here, we utilize genetic mAChR knockout animals in combination with nonselective mAChR antagonists to confirm that the M4 receptor activation is required for the locomotor-stimulating and antiparkinsonian efficacy in rodent models. We also report the synthesis, discovery, and characterization of the first-in-class selective M4 antagonists VU6013720, VU6021302, and VU6021625 and confirm that these optimized compounds have antiparkinsonian and antidystonic efficacy in pharmacol. and genetic models of movement disorders.
The article 《Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy》 also mentions many details about this compound(144230-52-4)COA of Formula: C5H10ClF2N, you can pay attention to it, because details determine success or failure
Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem