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1-[2-[BIS[4-(TRIFLUOROMETHYL)PHENYL]METHOXY]ETHYL]-1,2,5,6-TETRAHYDROPYRIDINE-3-CARBOXYLIC ACID HYDROCHLORIDE

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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-(TRIFLUOROMETHYL)PHENYL]METHOXY]ETHYL]-1,2,5,6-TETRAHYDROPYRIDINE-3-CARBOXYLIC ACID HYDROCHLORIDE
  • 1-[2-bis[4-(Trifluormethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine3-carboxylic acid hydrochloride
  • CI 966 hydrochlorid
CAS:
110283-66-4
MF:
C23H22ClF6NO3
MW:
509.87
Product Categories:
  • GABA/Glycine receptor
Mol File:
110283-66-4.mol
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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
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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.

storage

Desiccate at RT

1-[2-[BIS[4-(TRIFLUOROMETHYL)PHENYL]METHOXY]ETHYL]-1,2,5,6-TETRAHYDROPYRIDINE-3-CARBOXYLIC ACID HYDROCHLORIDESupplier

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1-[2-[BIS[4-(TRIFLUOROMETHYL)PHENYL]METHOXY]ETHYL]-1,2,5,6-TETRAHYDROPYRIDINE-3-CARBOXYLIC ACID HYDROCHLORIDE(110283-66-4)Related Product Information