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[CAS NO. 145821-59-6] Tiagabine hydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-B0696A |
| Brand: | MCE |
| CAS: | 145821-59-6 |
Overview
| MDL | MFCD07369025 |
|---|---|
| Molecular Weight | 412.01 |
| Molecular Formula | C20H26ClNO2S2 |
| SMILES | O=C([C@H]1CN(CC/C=C(C2=C(C)C=CS2)/C3=C(C)C=CS3)CCC1)O.[H]Cl |
Summary
Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC 50 s of 67, 446 and 182 nM for [ 3 H]GABA uptake in Synaptosomes, Neurons and Glia, respectively [1] .
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00086255 | National Institute on Drug Abuse (NIDA)|University of Cincinnati |
Cocaine-Related Disorders
|
October 2002 | Phase 2 |
| NCT00179465 | Beth Israel Deaconess Medical Center|Dartmouth-Hitchcock Medical Center |
Schizophrenia
|
November 2003 | Phase 3 |
| NCT00129298 | National Institute on Drug Abuse (NIDA) |
Cocaine-Related Disorders|Opiate Dependence
|
December 2004 | Phase 2 |
| NCT02387710 | Brigham and Women´s Hospital |
Sleep Apnea, Obstructive
|
March 2015 | Phase 2 |
| NCT03196466 | Assistance Publique - Hôpitaux de Paris |
Epilepsy
|
June 19, 2017 | |
| NCT01904487 | Rajesh Narendran|University of Pittsburgh |
Alcoholism
|
April 19, 2011 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 242.71 mM ; Need ultrasonic)
DMSO : ≥ 53 mg/mL ( 128.64 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4271 mL | 12.1356 mL | 24.2713 mL |
| 5 mM | 0.4854 mL | 2.4271 mL | 4.8543 mL |
| 10 mM | 0.2427 mL | 1.2136 mL | 2.4271 mL |
References
- [1] Braestrup C, et al. (R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid binds with high affinity to the brain gamma-aminobutyric acid uptake carrier. J Neurochem. 1990 Feb;54(2):639-47.
- [2] Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40(3): p. 32-40.
- [3] Henjum, S. and B. Hassel, High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int, 2007. 50(2): p. 365-70.
Synonyms
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