Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H18FN3.ClH |
Molecular Weight | 319.804 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCCN(N1C=C(C)C2=C1C=CC=C2)C3=CC=NC=C3F
InChI
InChIKey=FYIIKHJFVLTAFI-UHFFFAOYSA-N
InChI=1S/C17H18FN3.ClH/c1-3-10-20(17-8-9-19-11-15(17)18)21-12-13(2)14-6-4-5-7-16(14)21;/h4-9,11-12H,3,10H2,1-2H3;1H
Molecular Formula | C17H18FN3 |
Molecular Weight | 283.3433 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Nerispirdine, an acetylcholine release enhancer and a K+/Na+ use-dependent channel blocker, was in clinical development with sanofi-aventis for the treatment of multiple sclerosis. Nerispirdine is not proconvulsant. It can inhibit axonal K(+) channels and this mechanism may underlie the ability of the drug to enhance neuronal conduction. Nerispirdine can also inhibit neuronal Na(+) channels, a mechanism that may explain why nerispirdine lacks proconvulsant activity.
Originator
Approval Year
Sample Use Guides
Visual function in patients with multiple sclerosis: single oral doses of 50 mg and 400 mg Nerispirdine
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19413590
Curator's Comment: Using whole-cell patch-clamp electrophysiology, the effects of nerispirdine on the cloned human K(+) channels K(v)1.1 and K(v)1.2, expressed in Chinese hamster ovary cells, and on voltage-dependent Na(+) channels recorded from human SH-SY5Y cells, were compared.
Nerispirdine inhibited K(v)1.1 and K(v)1.2 with IC(50) values of 3.6 and 3.7 umol/L, respectively. Nerispirdine also inhibited voltage-dependent Na(+) channel currents recorded from human SH-SY5Y cells with an IC(50) of 11.9 umol/L when measured from a -70 mV holding potential.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:52:31 GMT 2023
by
admin
on
Fri Dec 15 15:52:31 GMT 2023
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Record UNII |
NK9ZSB7Q1G
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Record Status |
Validated (UNII)
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Record Version |
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9818503
Created by
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NK9ZSB7Q1G
Created by
admin on Fri Dec 15 15:52:31 GMT 2023 , Edited by admin on Fri Dec 15 15:52:31 GMT 2023
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119229-64-0
Created by
admin on Fri Dec 15 15:52:31 GMT 2023 , Edited by admin on Fri Dec 15 15:52:31 GMT 2023
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Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE |