1、GBR 12935 dihydrochlorideCat. No.: HY-12242CAS No.: 67469-81-2Molecular Formula: CHClNOMolecular Weight: 487.5Target: Dopamine TransporterPathway: Neuronal SignalingStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent Need ultrasonic and warming)ConcentrationSolvent Mass
2、 1 mg 5 mg 10 mg1 mM 2.0513 mL 10.2564 mL 20.5128 mL5 mM 0.4103 mL 2.0513 mL 4.1026 mLPreparing Stock Solutions10 mM 0.2051 mL 1.0256 mL 2.0513 mLPlease refer to the solubility information to select the appropriate solvent.BIOLOGICAL ACTIVITYDescription GBR 12935 2Hcl is a potent, and selective dopa
3、mine reuptake inhibitor.IC50 value: Target: dopamine reuptake inhibitorin vitro: The calculated Kd of 3HGBR-12935 binding to CYP2D6 was 42.2 nM, indicating that GBR-12935 has a high affinity for CYP2D6. The binding of 3HGBR-12935 to CYP2D6 was decreased partially by substrates or inhibitors of CYP2D
4、 isoforms (quinine, quinidine, propranolol, bufuralol, imipramine, and desipramine) 1. Co-perfusion of 100 microM GBR 12909 or GBR 12935 with either 100 microM sulpiride or raclopride produced a significant reduction in the GBR 12909 or GBR 12935 induced increase in the extracellular levels of dopam
5、ine to basal levels. In vitro, GBR 12909 (1-9 nM) dose-dependently inhibited active uptake of 3Hdopamine in homogenates of the nucleus accumbens 2.in vivo: GBR 12935 elevated locomotion to a greater extent in C57BL/6J mice at the maximally active dose of 10 mg/kg. Locomotor stimulation by GBR 12935
6、remained consistent in both strains with repeated injections. DBA/2J mice became sensitized to cocaine-induced stereotypy with repeated injections. Cocaine induced no stereotypy in C57BL/6J mice on any test day. No stereotypies were induced by GBR 12935 in either strain on any test day 3.Product Dat
7、a Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1REFERENCES1. Hiroi T, et al. Specific binding of 1-2-(diphenylmethoxy)ethyl-4-(3-phenyl propyl) piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6. Biochem Pharmacol. 1997 Jun 15;53(12):1937-9.2. Rahman S, et al
8、. Negative interaction of dopamine D2 receptor antagonists and GBR 12909 and GBR 12935 dopamine uptake inhibitors in the nucleus accumbens. Eur J Pharmacol. 2001 Feb 23;414(1):37-44.3. Tolliver BK, et al. Comparison of cocaine and GBR 12935: effects on locomotor activity and stereotypy in two inbred mouse strains. Pharmacol Biochem Behav. 1994 Jul;48(3):733-9.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USAwww.MedChemE2
