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Discovery of diphenyl amine based sodium channel blockers, effective against hNav1

All Rights Reserved. Discovery of diphenyl amine based sodium channel blockers, effective against hNav1.2. Hudgens, Debjani P.; Taylor, Catherine; Batts, Timothy W.; Patel, Manoj K.; Brown, Milton L. (Department of Chemistry, University of Virginia, Charlottesville, VA 22904, USA). Bioorganic & Medicinal Chemistry, 14(24), 8366-8378 (English) 2006 Elsevier Ltd. CODEN: BMECEP. ISSN: 0968-0896. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 25 The development of new therapies for chronic pain is an area of unmet medical need. 109-54-6 which is the cas registry number is also used here. Central to pathways of chronic pain is the upregulation of voltage-gated sodium channels. The use of tricyclic antidepressants, which also have sodium channel activity, in chronic pain therapy prompted us to develop novel compds. from this scaffold. Herein, we show that the tricyclic moiety is not needed for effective inhibition of the [3H]-BTX binding site and sodium currents of hNav1.2. Our lead compd. 6 (I), contg. a di-Ph amine motif, demonstrated a 53% inhibitory block of Nav1.2 currents at 10 mM, which is greater than 50% increase in current block in comparison to the amitriptyline std. Altogether our study establishes that the tricyclic motif is unnecessary for hNav1.2 activity and modification of the amine portion is detrimental to sodium channel block. .