Linopirdine
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Linopirdine is a putative cognition-enhancing drug with a novel mechanism of action. Linopirdine blocks the KCNQ2\3 heteromer M current with an IC50 of 2.4 micromolar[1] disinhibiting acetylcholine release, and increasing hippocampal CA3-schaffer collateral mediated glutamate release onto CA1 pyramidal neurons.[2] In a murine model linopirdine is able to nearly completely reverse the senescence-related decline in cortical c-FOS, an effect which is blocked by atropine and MK-801, suggesting Linopirdine can compensate for the age related decline in acetylcholine release.[3] Linopirdine also blocks homomeric KCNQ1 and KCNQ4 voltage gated potassium channels which contribute to vascular tone with substantially less selectivity than KCNQ2/3.[1] Linopirdine also acts as a glycine receptor antagonist in concentrations typical for Kv7 studies in the brain.[4]
Synthesis
The amide formation between
References
- ^ PMID 9694925.
- PMID 22674722.
- S2CID 45164.
- S2CID 247231429.
- .
- S2CID 98146660.
- ^ US 4806651, Bryant III WM, Huhn GF, issued 1989, assigned to E.I. Du Pont De Nemours and Company
- ^ US 5173489, Earl RA, Myers MJ, Nickolson VJ, issued 1992, assigned to The Dupont Merck Pharmaceutical Co.