Linopirdine dihydrochloride

Cat. No. 1999

Linopirdine dihydrochloride C26H21N3O.2HCl [113168-57-3]

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Alternative Name: DuP 996

Chemical Name: 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one dihydrochloride

Biological Activity

Blocker of KV7 (KCNQ) voltage-gated potassium channels; blocks KV7.1+7.3 (KCNQ2+3) / M-currents (IC50 = 4 - 7 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 8.9 μM). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo.

Technical Data

M.Wt:
464.39
Formula:
C26H21N3O.2HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at RT
CAS No:
113168-57-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Schnee and Brown (1998) Selectivity of linopirdine (DuP 966), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J.Pharmacol.Exp.Ther. 286 709. PMID: 9694925.

Wang et al (1998) KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 282 1890. PMID: 9836639.

Zaczek et al (1998) Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine. J.Pharmacol.Exp.Ther. 285 724. PMID: 9580619.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Linopirdine dihydrochloride include:

Carrott et al (2016) Absence of Neuroplastin-65 Affects Synaptogenesis in Mouse Inner Hair Cells and Causes Profound Hearing Loss. J Pharmacol Exp Ther 36 222. PMID: 26740663.

Zampini et al (2013) Burst activity and ultrafast activation kinetics of CaV1.3 Ca2+ channels support presynaptic activity in adult gerbil hair cell ribbon synapses. Front Cell Neurosci 591 3811. PMID: 23713031.

Joshi et al (2009) KCNQ modulators reveal a key role for KCNQ potassium channels in regulating the tone of rat pulmonary artery smooth muscle. J Physiol 329 368. PMID: 19151245.

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Keywords: Linopirdine dihydrochloride, supplier, KCNQ, channel, blockers, Potassium, KV, kv7, Channels, voltage-gated, voltage-dependent, K+, KCNQ2, KCNQ3, KCNQ1, DuP996, Tocris Bioscience, Voltage-gated Potassium (KV) Channel Blocker products

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