GBR-12909 CAS: 67469-78-7
MF: C28H32F2N2O•2HCl
MW: 523.49
A potent dopamine transport blocker studied extensively in rats.

GBR-12909 (CAS 67469-78-7)

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Alternate Names: Vanoxerine dihydrochloride;1-(2-(bis-(4-Fluorophenyl)methoxy)ethyl)-4-(3-phenyl-2-propyl)piperazine 2HCl
Application GBR-12909 is a potent dopamine transport blocker studied extensively in rats
CAS 등록번호: 67469-78-7
순도: ≥98%
분자량: 523.49
분자식: C28H32F2N2O•2HCl
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
* 참조분석증명서대량의 측정 데이터(함수량포함).

GBR-12909 is a potent dopamine transport blocker studied extensively in rats. By inhibiting DAT function, GBR-12909 was able to induce bipolar disorder mania-like phenotypes in mice. Also shown to cause postnatal changes to produce useful ADHD animal models. GBR-12909 caused an increase in core body temperature when administered to serotonin transporter knockout mice. Reportedly mimics cocaine-mediated enhancement of Tat neurotoxicity in rat midbrain primary cell cultures. Analogs of GBR-12909 continue to be investigated for cocaine addiction treatments.


References

1. Rothman, R.B., et al. 2008. Biochem. Pharmacol. 75: 2-16. PMID: 17897630
2. Aksenov, M.Y., et al. 2008. Neurotoxicology. 29: 971-977. PMID: 18606182
3. Hewitt, K.N., et al. 2009. Neuropharmacology. 57: 678-686. PMID: 19699754
4. Young, J.W., et al. 2010. Psychopharmacology. 208: 443-454. PMID: 20020109

Physical State :
Solid
용해도 :
Soluble in DMSO (>5 mg/ml), water (25 mg/ml), methanol (25 mg/ml), and ethanol (4 mg/ml).
저장 :
Store at room temperature
IC50 :
sigma ligand: IC50 = 48 nM; Dopamine transporter: IC50 = 6.63 nM (Rattus norvegicus); Serotonin transporter: IC50 = 132 nM (Rattus norvegicus); Norepinephrine transporter: IC50 = 496 nM (Rattus norvegicus); Danio rerio: IC50 = 5730 nM
Ki 데이타 :
Dopamine transporter: Ki= 3.7 nM (Rattus norvegicus); Striatal dopamine uptake: Ki= 1 nM
pK Values :
pKb: 7.55
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
WGK Germany :
3
RTECS :
TB9659030
PubChem CID :
MDL Number :
MFCD00055193
SMILES :
C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl

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GBR-12909 (CAS 67469-78-7)  논문정보

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PMID: # 18845198  Stepanov, V. et al. 2008. Neurochem. Int. 53: 370-373.

PMID: # 1678014  Melia, KF. et al. 1991. J. Pharmacol. Exp. Ther. 258: 626-632.

PMID: # 2430678  Teicher, MH. et al. 1986. Brain Res. 395: 124-128.

PMID: # 6237922  Heikkila, RE. et al. 1984. Eur. J. Pharmacol. 103: 241-248.

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