1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE
- CAS No.
- 105431-72-9
- Chemical Name:
- 1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE
- Synonyms
- linopiridine;Linopirdine2HCl;LINOPIRDINE (DUP996);LINOPIRDINE DIHYDROCHLORIDE;1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one;1-phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one;1-Phenyl-3,3-bis(4-pyridinylmethyl)-2,3-dihydro-1H-indole-2-one;2H-Indol-2-one, 1,3-dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-;1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one dihydrochloride;1,3-Dihydro-1-Phenyl-3,3-Bis(4-Pyridinylmethyl)-2H-Indol-2-One(WXC03502)
- CBNumber:
- CB6283722
- Molecular Formula:
- C26H21N3O
- Molecular Weight:
- 391.46
- MOL File:
- 105431-72-9.mol
- Modify Date:
- 2023/5/18 11:31:19
Melting point | 186-186.5 °C |
---|---|
Boiling point | 655.9±50.0 °C(Predicted) |
Density | 1?+-.0.06 g/cm3(Predicted) |
storage temp. | Desiccate at RT |
solubility | DMSO: >10mg/mL |
pka | 6.01±0.10(Predicted) |
form | A crystalline solid |
color | white to off-white |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H302-H315-H319-H335 |
Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501 |
WGK Germany | 3 |
1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE price More Price(2)
1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE Chemical Properties,Uses,Production
Description
Linopirdine is an enhancer of the stimulus-evoked but not basal release of several neurotransmitters, including acetylcholine, dopamine, serotonin, and glutamate. It increases acetylcholine release in rat hippocampal CA1 neurons by blocking voltage-gated, calcium-activated and leak (M-type; Kv7.2/7.3; KCNQ2/3) K+ current with an IC50 value of 2.4 μM. Inhibition of M-channels is reported to result in the depolarization of CA3 pyramidal neurons and activated presynaptic voltage-gated P/Q- and N-type calcium channels, which leads to Ca2+ influx and increased neurotransmitter release. Linopirdine has been shown to produce a number of effects including EEG patterns of enhanced vigilance, induction of c-fos expression in cerebral cortex, reduction of the increase of cerebral glucose utilization induced by hypoxia, and improved performance in animal models of learning and memory. Linopirdine has also been identified as an agonist of transient receptor potential vanilloid type 1 (EC50 = 115 μM in HEK293 cells voltage clamped at -60 mV).
Uses
Alzheimer’s disease treatment (cognition enhancer).
Biological Activity
Blocker of KCNQ voltage-gated potassium channels; blocks KCNQ2+3/M-currents (IC 50 = 4-7 μ M) and KCNQ1 homomeric channels (IC 50 = 8.9 μ M). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo .
1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE Preparation Products And Raw materials
Raw materials
Preparation Products
1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE Suppliers
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