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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 2.4nM<ref name="pmid9694925">{{Cite pmid|9694925}}</ref> disinhibiting acetylcholine release, and increasing hippocampal CA3-schaffer collateral mediated glutamate release onto CA1 pyramidal neurons.<ref name="pmid22674722">{{Cite pmid|22674722}}</ref> 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.<ref name="pmid11378256">{{Cite pmid|11378256}}</ref> Linopirdine also blocks homomeric KCNQ1 and KCNQ4 voltage gated potassium channels which contribute to vascular tone with substantially less selectivity than KCNQ2/3.<ref name="pmid9694925">{{Cite pmid|9694925}}</ref>
'''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<ref name="pmid9694925">{{Cite journal
| last1 = Schnee | first1 = M. E.
| last2 = Brown | first2 = B. S.
| title = Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons
| journal = The Journal of pharmacology and experimental therapeutics
| volume = 286
| issue = 2
| pages = 709–717
| year = 1998
| pmid = 9694925
}}</ref> disinhibiting acetylcholine release, and increasing hippocampal CA3-schaffer collateral mediated glutamate release onto CA1 pyramidal neurons.<ref name="pmid22674722">{{Cite journal
| last1 = Sun | first1 = J.
| last2 = Kapur | first2 = J.
| doi = 10.1113/jphysiol.2012.235820
| title = M-type potassium channels modulate Schaffer collateral-CA1 glutamatergic synaptic transmission
| journal = The Journal of Physiology
| volume = 590
| issue = 16
| pages = 3953–3964
| year = 2012
| pmid = 22674722
| pmc =3476642
}}</ref> 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.<ref name="pmid11378256">{{Cite journal
| last1 = Dent | first1 = G. W.
| last2 = Rule | first2 = B. L.
| last3 = Zhan | first3 = Y.
| last4 = Grzanna | first4 = R.
| title = The acetylcholine release enhancer linopirdine induces Fos in neocortex of aged rats
| journal = Neurobiology of aging
| volume = 22
| issue = 3
| pages = 485–494
| year = 2001
| pmid = 11378256 | doi=10.1016/s0197-4580(00)00252-9
}}</ref> Linopirdine also blocks homomeric KCNQ1 and KCNQ4 voltage gated potassium channels which contribute to vascular tone with substantially less selectivity than KCNQ2/3.<ref name="pmid9694925">{{Cite journal
| last1 = Schnee | first1 = M. E.
| last2 = Brown | first2 = B. S.
| title = Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons
| journal = The Journal of pharmacology and experimental therapeutics
| volume = 286
| issue = 2
| pages = 709–717
| year = 1998
| pmid = 9694925
}}</ref>


==References==
==References==

Revision as of 22:24, 27 August 2015

Linopirdine
Clinical data
ATC code
Identifiers
  • 1-phenyl-3,3-bis(pyridin-4-ylmethyl)-1,3-dihydro-2H-indol-2-one
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H21N3O
Molar mass391.465 g/mol g·mol−1
3D model (JSmol)
  • O=C2N(c1ccccc1C2(Cc3ccncc3)Cc4ccncc4)c5ccccc5
  • 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 checkY
  • Key:YEJCDKJIEMIWRQ-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

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 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]

References

  1. ^ a b Schnee, M. E.; Brown, B. S. (1998). "Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons". The Journal of pharmacology and experimental therapeutics. 286 (2): 709–717. PMID 9694925.
  2. ^ Sun, J.; Kapur, J. (2012). "M-type potassium channels modulate Schaffer collateral-CA1 glutamatergic synaptic transmission". The Journal of Physiology. 590 (16): 3953–3964. doi:10.1113/jphysiol.2012.235820. PMC 3476642. PMID 22674722.
  3. ^ Dent, G. W.; Rule, B. L.; Zhan, Y.; Grzanna, R. (2001). "The acetylcholine release enhancer linopirdine induces Fos in neocortex of aged rats". Neurobiology of aging. 22 (3): 485–494. doi:10.1016/s0197-4580(00)00252-9. PMID 11378256.

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