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| | 1-[2-[Bis[4-(trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride Basic information |
| Product Name: | 1-[2-[Bis[4-(trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride | | Synonyms: | 1-[2-[bis[4-(trifluoromethyl)phenyl]methoxy]ethyl]-3,6-dihydro-2H-pyridine-5-carboxylic acid hydrochloride;3-pyridinecarboxylicacid,1,2,5,6-tetrahydro-1-(2-(bis(4-(trifluoromethyl)phen;ci966;CI 966 HYDROCHLORIDE;1-[2-[BIS(4-(TRIFLUOROMETHYL)PHENYL)METHOXY]ETHYL]-1,2,5,6-TETRAHYDROPYRIDINE-3-CARBOXYLIC ACID;1-[2-bis[4-(Trifluormethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine3-carboxylic acid hydrochloride;CI 966 hydrochlorid;1-(2-(Bis(4-(trifluoromethyl)phenyl)methoxy)ethyl)-1,2,5,6-tetrahydropyridine-3-carboxylicacidhydrochloride | | CAS: | 110283-66-4 | | MF: | C23H22ClF6NO3 | | MW: | 509.87 | | EINECS: | | | Product Categories: | GABA/Glycine receptor | | Mol File: | 110283-66-4.mol | ![1-[2-[Bis[4-(trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride Structure](CAS/GIF/110283-66-4.gif) |
| | 1-[2-[Bis[4-(trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride Chemical Properties |
| Melting point | 240-244 °C | | storage temp. | Desiccate at RT | | solubility | Soluble to 10 mM in ethanol and to 100 mM in DMSO | | form | Solid | | color | White to off-white |
| | 1-[2-[Bis[4-(trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride Usage And Synthesis |
| Uses | CI-966 Hydrochloride is highly selective for the cloned GABA transporter GAT-1. CI 966 Hydrochloride is a GABA transport inhibitor. | | Biological Activity | Selective inhibitor of the GABA transporter GAT-1 (IC 50 values are 0.26 and 1.2 μ M at cloned human and rat GAT-1 respectively). Displays over 200-fold selectivity over GAT-2 and GAT-3. Centrally active upon systemic administration in vivo . Anticonvulsive and neuroprotective. | | in vivo | CI-966 hydrochloride produces intermediate levels of Pentylenetetrazol (PTZ)-lever responding when administered to PTZ-trained rats[4].
CI-966 hydrochloride enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. CI-966 hydrochloride is administered systemically by i.p. injection (5 mg/kg) in Sprague-Dawley rats under urethane anaesthesia. Twenty to thirty minutes after injection there is a highly variable, but overall significant, enhancement of the inhibition of hippocampal population spikes by GABA applied by microiontophoresis in the CA1 region[5].
CI-966 hydrochloride exhibits anticonvulsant properties in various animal models. Oral absorption of CI-966 hydrochloride in dogs given 1.39 mg/kg is rapid with a tmax of 0.7 hr.
In rats given 5 mg/kg oral, a mean tmax of 4.0 hr is observed. Following i.v. administration of the same respective doses, elimination t1/2 in dogs and rats averages 1.2 and 4.5 hr. Absolute oral bioavailability of CI-966 hydrochloride is 100% in both species[6]. | Animal Model: | Eight male Sprague-Dawley rats[4] | | Dosage: | 0.3-30 mg/kg | | Administration: | Injection IP in a volume of 1 mL/kg | | Result: | Dose dependent decreases in rates of responding occurred following CI-966 administration.
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| | storage | Desiccate at RT |
| | 1-[2-[Bis[4-(trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride Preparation Products And Raw materials |
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