| dbo:abstract |
Linopirdin (DuP996) ist ein vom amerikanischen Konzern DuPont entwickeltes und 1990 vorgestelltes Molekül. Es verstärkt die Ausschüttung von Neurotransmittern und blockiert direkt spannungsabhängige Kaliumkanäle. Es ist ein Vertreter der Nootropika, einer Klasse Wirkstoffe, die vorteilhaft auf das Zentralnervensystem wirken, und wurde – allerdings ergebnislos – als möglicher Wirkstoff gegen die Alzheimer-Krankheit untersucht. (de) 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 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. (en) |
| dbo:casNumber |
105431-72-9 |
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319111 |
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D04741 |
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https://pubchem.ncbi.nlm.nih.gov/compound/10358387 https://pubchem.ncbi.nlm.nih.gov/compound/10470081 https://pubchem.ncbi.nlm.nih.gov/compound/11594101 |
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| rdfs:comment |
Linopirdin (DuP996) ist ein vom amerikanischen Konzern DuPont entwickeltes und 1990 vorgestelltes Molekül. Es verstärkt die Ausschüttung von Neurotransmittern und blockiert direkt spannungsabhängige Kaliumkanäle. Es ist ein Vertreter der Nootropika, einer Klasse Wirkstoffe, die vorteilhaft auf das Zentralnervensystem wirken, und wurde – allerdings ergebnislos – als möglicher Wirkstoff gegen die Alzheimer-Krankheit untersucht. (de) 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 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. (en) |
| rdfs:label |
Linopirdin (de) Linopirdine (en) |
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