TTA-P2
Based on 2 publication(s) in Google Scholar
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>[4].
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- 純度: 99.58%
- CAS 番号: 1072018-68-8
- 分子式: C21H29Cl2FN2O2
- 分子量:431.37
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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MedChemExpress（MCE）の使用を引用している文献 TTA-P2
MoreCalcium Channel アイソフォーム固有の製品をすべて表示
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生物活性
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T-type calcium channel |
Cav3.2 |
TTA-P2 (1-10 μM) inhibits most of the T current recorded at the holding potentials of -90 mV, and the inhibitory effect has a fast onset but was slowly and partially reversible in dorsal root ganglion (DRG) cells[2].
TTA-P2 (3 μM, 10 min) has maximal effect within 3-4 min after application[3].
TTA-P2 (1 μM, 70 min) fully recovers the window component of the T-type Ca2+ current (IT) after 50 min of wash out in ventrobasal nucleus (VB) thalamocortical (TC) neurons[3].
TTA-P2 (1 nM-1 μM) blocks IT dose-dependently with an IC50 of 22 nM in VB TC neurons [3].
TTA-P2 (1 μM, 20 min) induces a maximal reduction of IT even in the absence of channel activation, indicating the absence of a use-dependent block in VB TC neurons [3].
TTA-P2 (25 nM, 20 min) induces a clear decrease in current amplitude with no apparent shift in the voltage dependence of channel activation and steady-state inactivation in VB TC neurons [3].
TTA-P2 (1 μM) decreases the amplitude of IT recorded in rat nucleus reticularis
thalami (NRT) neurons, whereas the high-voltage-activated (HVA) Ca2+ current in the same neurons is not affected[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TTA-P2 (5-7.5 mg/kg, i.p., single dose) significantly reduces licking and biting of the affected paws injected with formalin at 7.5 mg/kg in CaV3.2 knockout mice[2].
TTA-P2 (5-10 mg/kg, i.p., single dose) allows complete reversal of neuropathic hyperalgesia at 10 mg/kg in diabetic Streptozocin (HY-13753)-treated rats[2].
TTA-P2 (1-10 mg/kg, p.o., single dose) exhibits a dose- and exposure-dependent decrease in the total seizure time during the 4 h period following oral dosing, demonstrating robust CNS efficacy at 10 mg/kg with a plasma level of 1 μM in WAG/Rij rat model of absence epilepsy and significantly reduces tremor activity in a dose-dependent manner in rat harmaline model[5].
TTA-P2 (1.29-4.30 (mg/kg)/60 min, i.v. infusion) has no significant impact in mean arterial blood pressure, heart rate or ECG intervals in dog models[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley rats (males and females, 300–350 g) with spinal cord injury[1]
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Dosage:0.3, 1, 3, 10 mg/kg, one single dose
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Had no effects on the mechanical threshold both at 30 min and 1-hour post-injection.
Reduced the mechanical hypersensitivity that developed following spinal cord injury in male rats.
Induced a robust conditioned place preference (CPP) with an increase in the difference score in the TTA-P2-paired chamber of 62 s and a decrease in the vehicle-paired chamber of -39 s.
Showed that the spontaneous ongoing pain following SCI is sensitive to TTA-P2 in male rats.
Increased the mechanical threshold to 16 g at 30 min post-injection and to 18 g at 1-hour post-injection in female rats with 10 mg/kg dose.
Were effective in reducing the mechanical hypersensitivity that developed following spinal cord injury in both male and female rats.
Had small effects with an increase in the difference score in the TTA-P2-paired chamber of 36 s and a decrease in the vehicle-paired chamber of -25 s.
Showed that the spontaneous ongoing pain following SCI has little or no sensitivity to TTA-P2 in female rats.
化学情報
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CAS 番号 1072018-68-8
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性状 Solid
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分子量 431.37
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分子式 C21H29Cl2FN2O2
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Color Off-white to light yellow
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SMILES
CC(C)(OCC1)C[C@H]1CN2CCC(F)(CC2)CNC(C3=CC(Cl)=CC(Cl)=C3)=O
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別名
T-Type calcium channel inhibitor
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
2024 Aug 27;15(1):7369. PMID: 39191796 -
CNS Neurosci Ther
Serotonin (5-HT)2A/2C receptor agonist 2,5-dimethoxy-4-iodophenyl-2-aminopropane hydrochloride improves detrusor sphincter dyssynergia by inhibiting L-type voltage-gated calcium channels in spinal cord injured rats. [Abstract]2024 Aug;30(8):e14890. PMID: 39097910
溶剤 & 溶解度
DMSO : 25 mg/mL (57.95 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[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]
[4]. Nigam, A., et al., (2019). Inhibition of T-Type calcium channels in mEC layer II stellate neurons reduces neuronal hyperexcitability associated with epilepsy. Epilepsy research, 154, 132-138. [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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3182 mL | 11.5910 mL | 23.1820 mL | 57.9549 mL |
| 5 mM | 0.4636 mL | 2.3182 mL | 4.6364 mL | 11.5910 mL | |
| 10 mM | 0.2318 mL | 1.1591 mL | 2.3182 mL | 5.7955 mL | |
| 15 mM | 0.1545 mL | 0.7727 mL | 1.5455 mL | 3.8637 mL | |
| 20 mM | 0.1159 mL | 0.5795 mL | 1.1591 mL | 2.8977 mL | |
| 25 mM | 0.0927 mL | 0.4636 mL | 0.9273 mL | 2.3182 mL | |
| 30 mM | 0.0773 mL | 0.3864 mL | 0.7727 mL | 1.9318 mL | |
| 40 mM | 0.0580 mL | 0.2898 mL | 0.5795 mL | 1.4489 mL | |
| 50 mM | 0.0464 mL | 0.2318 mL | 0.4636 mL | 1.1591 mL |
TTA-P2 関連分類
HY-10035 関連分類
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