GBR 12935 dihydrochloride CAS: 67469-81-2
MF: C28H34N2O•2HCl
MW: 487.51
A DAT and SLC6A2 inhibitor.

GBR 12935 dihydrochloride (CAS 67469-81-2)

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Alternate Names: 1-(2-Diphenylmethoxyethyl)-4-(3-phenylpropyl)piperazine dihydrochloride
Application GBR 12935 dihydrochloride is a DAT and SLC6A2 inhibitor
CAS 등록번호: 67469-81-2
분자량: 487.51
분자식: C28H34N2O•2HCl
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
* 참조분석증명서대량의 측정 데이터(함수량포함).

GBR 12935 dihydrochloride inhibits DAT (dopamine transporter) (Ki = 21.5 nM) and SLC6A2 (norepinephrine transporter) (Ki = 225 nM). GBR 12935 does not inhibit the serotonin transporter (Ki = 6.5 μM). GBR 12935 binds to a nondopaminergic piperazine site in blood platelets and brain that has been identified as cytochrome P450.


References

Andersen et al (1987) Biochemical and pharmacological characterization of [3H]GBR 12935 binding in vitro to rat striatal membranes: labelling of the dopamine uptake complex. J.Neurochem. 48 1887. Reith et al (1992) Evidence for mutually exclusive binding of cocaine, BTCP, GBR 12935, and dopamine to the dopamine transporter. Eur.J.Pharmacol.Mol.Pharmacol.Sect. 227 417. Reith et al (1994) GBR 12909 and 12935 block dopamine uptake into brain synaptic vesicles as well as nerve endings. Eur.J.Pharmacol. 253 175.

Physical State :
Solid
용해도 :
Soluble in DMSO (5 mM), and water (20 mg/ml).
저장 :
Desiccate at -20° C
굴절률 :
n20D ~1.58 (Predicted)
Ki 데이타 :
Serotonin transporter: Ki= 6.5 µM
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
WGK Germany :
3
PubChem CID :
MDL Number :
MFCD00083175
SMILES :
C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=CC=C3)C4=CC=CC=C4.Cl.Cl

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분석증명서

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GBR 12935 dihydrochloride (CAS 67469-81-2)  논문정보

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PMID: # 33610553  Sorkina, T.|Cheng, MH.|Bagalkot, TR.|Wallace, C.|Watkins, SC.|Bahar, I.|Sorkin, A.| et al. 2021. J Biol Chem. 100430.

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