CI-966 (hydrochloride)

CI-966 hydrochloride 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 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities[1][2][3].

Product Specifications

CAS Number

[110283-66-4]

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ci-966-hydrochloride.html

Purity

99.60

Solubility

DMSO : 50 mg/mL (ultrasonic)

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.[H]Cl

Molecular Formula

C23H22ClF6NO3

Molecular Weight

509.87

Precautions

H302, H312, H332

References & Citations

[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.|[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.|[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.|[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.|[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.|[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.