Linopirdine

Linopirdine

Gene therapy
Clinical data
ATC code	N06BX09 (WHO)
Physiological data
Legal status
Pharmacokinetic data
Identifiers
IUPAC name 1-phenyl-3,3-bis(pyridin-4-ylmethyl)-1,3-dihydro-2H-indol-2-one
CAS Number	105431-72-9 N
PubChem Template:Abbreviation	3932
IUPHAR/BPS	2599
ChemSpider	3795 Y
UNII	I5TB3NZ94T
KEGG	D04741 Y
ChEMBL	ChEMBL319111 Y
Chemical and physical data
Formula	C26H21N3O
Molar mass	391.465 g/mol
3D model (JSmol)	Interactive image
SMILES O=C2N(c1ccccc1C2(Cc3ccncc3)Cc4ccncc4)c5ccccc5
InChI InChI=1S/C26H21N3O/c30-25-26(18-20-10-14-27-15-11-20,19-21-12-16-28-17-13-21)23-8-4-5-9-24(23)29(25)22-6-2-1-3-7-22/h1-17H,18-19H2 Y Key:YEJCDKJIEMIWRQ-UHFFFAOYSA-N Y
Template:XmarkY (what is this?)  (verify)

WikiDoc Resources for Linopirdine
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Evidence Based Medicine
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Definitions
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Experimental / Informatics
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

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 2.4nM disinhibiting acetylcholine release, and increasing hippocampal CA3-schaffer collateral mediated glutamate release onto CA1 pyramidal neurons. 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. Linopirdine also blocks homomeric KCNQ1 and KCNQ4 voltage gated potassium channels which contribute to vascular tone with substantially less selectivity than KCNQ2/3.