User:Viralmemesis/sandbox
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,[1] disinhibiting acetylcholine release, and increases hippocampal CA3-schaffer collateral glutamate release onto CA1 pyramidal neurons.[2] Linopirdine is able to nearly completely reverse the senescence-related decline in cortical c-FOS, this effect 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]
- ^ a b Schnee ME, Brown BS (1998) Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J Pharmacol Exp Ther 286 (2):709-17. PMID: 9694925
- ^ Sun J, Kapur J (2012) M-type potassium channels modulate Schaffer collateral-CA1 glutamatergic synaptic transmission. J Physiol 590 (Pt 16):3953-64. DOI:10.1113/jphysiol.2012.235820 PMID: 22674722
- ^ Dent GW, Rule BL, Zhan Y, Grzanna R (2001) The acetylcholine release enhancer linopirdine induces Fos in neocortex of aged rats. Neurobiol Aging 22 (3):485-94. PMID: 11378256