| Identification | Back Directory | [Name]
1-[2-[BIS[4-(TRIFLUOROMETHYL)PHENYL]METHOXY]ETHYL]-1,2,5,6-TETRAHYDROPYRIDINE-3-CARBOXYLIC ACID HYDROCHLORIDE | [CAS]
110283-66-4 | [Synonyms]
ci966
CI966HCl
CI 966 hydrochlorid
CI 966 HYDROCHLORIDE
CI-966 hydrochloride
(CI966)
3-pyridinecarboxylicacid,1,2,5,6-tetrahydro-1-(2-(bis(4-(trifluoromethyl)phen
1-[2-[BIS(4-(TRIFLUOROMETHYL)PHENYL)METHOXY]ETHYL]-1,2,5,6-TETRAHYDROPYRIDINE-3-CARBOXYLIC ACID
1-[2-[bis[4-(trifluoromethyl)phenyl]methoxy]ethyl]-3,6-dihydro-2H-pyridine-5-carboxylic acid hydrochloride
1-[2-bis[4-(Trifluormethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine3-carboxylic acid hydrochloride
1-(2-(Bis(4-(trifluoromethyl)phenyl)methoxy)ethyl)-1,2,5,6-tetrahydropyridine-3-carboxylicacidhydrochloride
1-[2-[BIS[4-(TRIFLUOROMETHYL)PHENYL]METHOXY]ETHYL]-1,2,5,6-TETRAHYDROPYRIDINE-3-CARBOXYLIC ACID HYDROCHLORIDE | [Molecular Formula]
C23H22ClF6NO3 | [MDL Number]
MFCD00889186 | [MOL File]
110283-66-4.mol | [Molecular Weight]
509.87 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
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