Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-Trifluoromethoxy N-Benzyl Isatins was written by Bridges, Thomas M.;Marlo, Joy E.;Niswender, Colleen M.;Jones, Carrie K.;Jadhav, Satyawan B.;Gentry, Patrick R.;Plumley, Hyekyung C.;Weaver, C. David;Conn, P. Jeffrey;Lindsley, Craig W.. And the article was included in Journal of Medicinal Chemistry in 2009.Formula: C7H5ClF2 This article mentions the following:
This report describes the discovery and initial characterization of the first pos. allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS identified VU0119498 (I), which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca2+ mobilization assays. Subsequent optimization led to the discovery of VU0238429 (II), which possessed an EC50 of approx. 1.16 μM at M5 with >30-fold selectivity vs. M1 and M3, with no M2 or M4 potentiator activity. In the experiment, the researchers used many compounds, for example, 2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4Formula: C7H5ClF2).
2-(Chloromethyl)-1,3-difluorobenzene (cas: 697-73-4) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Formula: C7H5ClF2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics