GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. It was originally developed in its 3H radiolabelled form for the purpose of mapping the distribution of dopaminergic neurons in the brain by selective labelling of dopamine transporter proteins. This has led to potential clinical uses in the diagnosis of Parkinson's disease, although selective radioligands such as Ioflupane (¹²³I) are now available for this application. GBR-12935 is now widely used in animal research into Parkinson's disease and the dopamine pathways in the brain.
Chemical Formula: C28H36Cl2N2O
Molecular Weight: 487.509
Elemental Analysis: C, 68.98; H, 7.44; Cl, 14.54; N, 5.75; O, 3.28
1-(2 (Diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride
InChi Code: InChI=1S/C28H34N2O.2ClH/c1-4-11-25(12-5-1)13-10-18-29-19-21-30(22-20-29)23-24-31-28(26-14-6-2-7-15-26)27-16-8-3-9-17-27;;/h1-9,11-12,14-17,28H,10,13,18-24H2;2*1H
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Sato T, Kitayama S, Morita K, Ikeda T, Dohi T. Changes in seizure susceptibility to local anesthetics by repeated administration of cocaine and nomifensine but not GBR12935: possible involvement of noradrenergic system. Jpn J Pharmacol. 2000 Jul;83(3):265-8. PubMed PMID: 10952077.
Bowden C, Cheetham SC, Lowther S, Katona CL, Crompton MR, Horton RW. Dopamine uptake sites, labelled with [3H]GBR12935, in brain samples from depressed suicides and controls. Eur Neuropsychopharmacol. 1997 Nov;7(4):247-52. PubMed PMID: 9443655.
Akunne HC, Dersch CM, Cadet JL, Baumann MH, Char GU, Partilla JS, de Costa BR, Rice KC, Carroll FI, Rothman RB. Studies of the biogenic amine transporters. III. Demonstration of two binding sites for [3H]GBR12935 and [3H]BTCP in rat caudate membranes. J Pharmacol Exp Ther. 1994 Mar;268(3):1462-75. PubMed PMID: 7908058.
Rothman RB, Lewis B, Dersch C, Xu H, Radesca L, de Costa BR, Rice KC, Kilburn RB, Akunne HC, Pert A. Identification of a GBR12935 homolog, LR1111, which is over 4,000-fold selective for the dopamine transporter, relative to serotonin and norepinephrine transporters. Synapse. 1993 May;14(1):34-9. PubMed PMID: 8511716.
Sharif NA, Nunes JL, Kalfayan V, McClelland DL, Rosenkranz RP, Eglen RM, Whiting RL. A pharmacological comparison of [3H]GBR12935 binding to rodent striatal and kidney homogenates: binding to dopamine transporters? Neurochem Int. 1992 Jul;21(1):69-73. PubMed PMID: 1303143.
Le WD, Bostwick JR, Appel SH. Use of [3H]-GBR12935 to measure dopaminergic nerve terminal growth into the developing rat striatum. Brain Res Dev Brain Res. 1992 Jun 19;67(2):375-7. PubMed PMID: 1511527.
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