1199236-64-0

Z944 is an inhibitor of T-type calcium channels (IC₅₀s = 0.050-0.160 μM for the human recombinant voltage-gated calcium (Ca_v) channels Ca_v3.1, Ca_v3.2, and Ca_v3.3). It is selective for T-type channels over the N-type Ca_v2.2 channel (IC₅₀ = 11 μM), as well as the rat L-type Ca_v1.2, human-ether-a-go-go (hERG/K_v11.1) potassium, and human voltage-gated sodium (Na_v) channel Na_v1.5 (IC₅₀s = 32, 7.8, and 100 μM, respectively). Z944 (30 mg/kg) reduces the seizure duration and the amount of time rats spend in seizures in a model of absence epilepsy. It delays seizure progression in amygdala-kindled rats but does not inhibit seizures in fully kindled rats.

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As N-Piperidinyl acetamide derivatives, N-((1-(2-(tert-ButylaMino)-2-oxoethyl)piperidin-4-yl)Methyl)-3-chloro-5-fluorobenzaMide can be used as calcium channel blockers and their use in the treatment of obesity.

ChEBI: Ulixacaltamide is a member of piperidines, a member of benzamides, a member of monochlorobenzenes, a member of monofluorobenzenes and a secondary carboxamide. It has a role as a T-type calcium channel blocker and a non-narcotic analgesic.

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[1] ELIZABETH TRINGHAM. T-Type Calcium Channel Blockers That Attenuate Thalamic Burst Firing and Suppress Absence Seizures[J]. Science Translational Medicine, 2012, 4 121. DOI: 10.1126/scitranslmed.3003120
[2] PABLO MIGUEL CASILLAS-ESPINOSA. Z944, a Novel Selective T-Type Calcium Channel Antagonist Delays the Progression of Seizures in the Amygdala Kindling Model.[J]. PLoS ONE, 2015: e0130012. DOI: 10.1371/journal.pone.0130012