CI-966
CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities.
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- CAS No.: 110283-79-9
- 화학식: C23H21F6NO3
- 분자량:473.41
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
IC50: 0.26 μM (hGAT-1); 1.2 μM (rGAT-1); 297 μM (rGAT-2); 333 μM (hGAT-3); 1140 μM (rGAT-3); 300 μM (hBGT-3)[1]
CI-966 functions by selectively inhibiting GABA reuptake in neurons and glial cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CI-966 enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. CI-966 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 exhibits anticonvulsant properties in various animal models. Oral absorption of CI-966 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 is 100% in both species[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight male Sprague-Dawley rats[4]
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Dosage:0.3-30 mg/kg
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Administration:Injection IP in a volume of 1 mL/kg
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Result:Dose dependent decreases in rates of responding occurred following CI-966 administration.
Chemical Information
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CAS No. 110283-79-9
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분자량 473.41
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화학식 C23H21F6NO3
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SMILES
O=C(C1=CCCN(CCOC(C2=CC=C(C(F)(F)F)C=C2)C3=CC=C(C(F)(F)F)C=C3)C1)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Borden LA, et, al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24. [Content Brief]
[2]. Green AR, et, al. GABA potentiation: a logical pharmacological approach for the treatment of acute ischaemic stroke. Neuropharmacology. 2000 Jul 10;39(9):1483-94. [Content Brief]
[3]. T G Dhar, et al. Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J Med Chem (IF: 7.45; Q1). 1994 Jul 22;37(15):2334-42. [Content Brief]
[4]. D M Grech, et al. Discriminative stimulus effects of presynaptic GABA agonists in pentobarbital-trained rats. Pharmacol Biochem Behav.1994 Jan;47(1):5-11. [Content Brief]
[5]. U Ebert, et al. Systemic CI-966, a new gamma-aminobutyric acid uptake blocker, enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. Can J Physiol Pharmacol. 1990 Sep;68(9):1194-9. [Content Brief]
[6]. L L Radulovic, et al. Pharmacokinetics, mass balance, and induction potential of a novel GABA uptake inhibitor, CI-966 HCl, in laboratory animals. Pharm Res. 1993 Oct;10(10):1442-5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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