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SML2635

Sigma-Aldrich

Z944 hydrochloride

≥98% (HPLC)

Synonym(e):

4-[[(3-Chloro-5-fluorobenzoyl)amino]methyl]-N-(1,1-dimethylethyl)-1-piperidineacetamide hydrochloride, N-((1-(2-(tert-Butylamino)-2-oxoethyl)piperidin-4-yl)methyl)-3-chloro-5-fluorobenzamide hydrochloride, Z 944 hydrochloride, Z-944

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About This Item

Empirische Formel (Hill-System):
C19H27ClFN3O2 · xHCl
Molekulargewicht:
383.89 (free base basis)
UNSPSC-Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Lagerbedingungen

desiccated

Farbe

white to beige

Löslichkeit

H2O: 2 mg/mL, clear

Lagertemp.

2-8°C

Biochem./physiol. Wirkung

Z944 is an orally available, state-dependent, potent and selective T-type calcium channel blocker (hCav3.1/Cav3.2/Cav3.3 IC50 by voltage clamp = 50/160/110 nM under ~30% inactivated state & 130/540/260 nM in the closed state) over non-T-type voltage-gated channels (rCaV2.2 IC50 = 11 μM/30% inactivated & 150 μM/closed; hERG/rCaV1.2/hNaV1.5 IC50 = 7.8/32/100 μM). Z944 effectively suppresses seizure activity in the GAERS (absence epilepsy rats from Strasbourg) model in vivo (10-30 mg/kg qod ip.) with no adverse cardiovascular effects or neurotoxicity.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

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Lina A Matschke et al.
Molecular and cellular neurosciences, 88, 330-341 (2018-03-11)
The physiological, intrinsic activity of noradrenergic locus coeruleus (LC) neurons is important for the control of sleep/wakefulness, cognition and autonomous body functions. Dysregulations of the LC-noradrenergic network contribute to the pathogenesis of psychiatric disorders and are key findings in early
Wendie N Marks et al.
Neuroscience, 332, 121-129 (2016-07-02)
The role of T-type calcium channels in brain diseases such as absence epilepsy and neuropathic pain has been studied extensively. However, less is known regarding the involvement of T-type channels in cognition and behavior. Prepulse inhibition (PPI) is a measure
Mark T Henbid et al.
Experimental neurology, 296, 16-22 (2017-06-29)
Childhood absence epilepsy (CAE) is associated with interictal co-morbid symptoms including abnormalities in social behaviour. Genetic Absence Epilepsy Rats from Strasbourg (GAERS) is a model of CAE that exhibits physiological and behavioural alterations characteristic of the human disorder. However, it
Andrew J Roebuck et al.
Psychopharmacology, 235(11), 3339-3350 (2018-09-27)
Currently available antipsychotics are unsatisfactory given their side effects and limited efficacy for the cognitive symptoms of schizophrenia. Many currently available drugs, such as haloperidol, are T-type calcium channel antagonists in addition to their well-established antagonism of dopamine D2 receptors.
Dongyang Huang et al.
Antioxidants & redox signaling, 25(5), 233-251 (2016-06-17)
Neuropeptide substance P (SP) is produced and released by a subset of peripheral sensory neurons that respond to tissue damage (nociceptors). SP exerts excitatory effects in the central nervous system, but peripheral SP actions are still poorly understood; therefore, here
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