1072018-68-8
Chemical Structure
TTA-P2
Synonym(s): T-Type calcium channel inhibitor
- CAS No.: 1072018-68-8
- Formula:C21H29Cl2FN2O2
- Molecular Weight:431.37
IUPAC Name: (S)-3,5-dichloro-N-((1-((2,2-dimethyltetrahydro-2H-pyran-4-yl)methyl)-4-fluoropiperidin-4-yl)methyl)benzamide
InChIKey: DKNDOKIVCXTFHJ-HNNXBMFYSA-N
SMILES: CC(C)(OCC1)C[C@H]1CN2CCC(F)(CC2)CNC(C3=CC(Cl)=CC(Cl)=C3)=O
Biological Activity: TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy[1][2][3]< sup>[4][5].
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TTA-P2 | 99.58% | TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy< sup>. | ||||||||||||||||||||
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TTA-P2 (Standard) | ≥98% | TTA-P2 (Standard) is the analytical standard of TTA-P2 (HY-10035). This product is intended for research and analytical applications. TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy< sup>. | ||||||||||||||||||||
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References
- [1]. Huilin Liu, et al., Inhibition of T-Type Calcium Channels With TTA-P2 Reduces Chronic Neuropathic Pain Following Spinal Cord Injury in Rats, The Journal of Pain, Volume 24, Issue 9, 2023, Pages 1681-1695, ISSN 1526-5900. [Content Brief]
- [2]. WonJoo Choe, et al., TTA-P2 Is a Potent and Selective Blocker of T-Type Calcium Channels in Rat Sensory Neurons and a Novel Antinociceptive Agent, Molecular Pharmacology, Volume 80, Issue 5, 2011, Pages 900-910, ISSN 0026-895X. [Content Brief]
- [3]. Dreyfus, F. M., et al., (2010). Selective T-type calcium channel block in thalamic neurons reveals channel redundancy and physiological impact of I(T)window. The Journal of neuroscience : the official journal of the Society for Neuroscience, 30(1), 99-109. [Content Brief]
- [5]. Shipe, W. D., et al., (2008). Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist. Journal of medicinal chemistry, 51(13), 3692-3695. [Content Brief]
