WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 574707
CAS#: 67469-75-4
Description: GBR-12783 dihydrochloride is a Dopamine uptake inhibitor.
MedKoo Cat#: 574707
Name: GBR-12783 dihydrochloride
CAS#: 67469-75-4
Chemical Formula: C28H34Cl2N2O
Exact Mass:
Molecular Weight: 485.493
Elemental Analysis: C, 69.27; H, 7.06; Cl, 14.60; N, 5.77; O, 3.30
Synonym: GBR-12783 dihydrochloride; GBR-12783 2HCl
IUPAC/Chemical Name: 1-(2-Benzhydryloxy-ethyl)-4-((E)-3-phenyl-allyl)-piperazine dihydrochloride
InChi Key: HJDXBLLTRMCYNC-JFXLULTRSA-N
InChi Code: InChI=1S/C28H32N2O.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;;/h1-17,28H,18-24H2;2*1H/b13-10+;;
SMILES Code: [H]Cl.[H]Cl.N1(CCOC(C2=CC=CC=C2)C3=CC=CC=C3)CCN(C/C=C/C4=CC=CC=C4)CC1
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: >3 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
| Biological target: | GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. |
| In vitro activity: | TBD |
| In vivo activity: | GBR-12783 (6 mg/Kg) reduced the immobility time (Fig. 4c) and increased the stepping activity (Fig. 4d) in WT but not G2019S KI mice, while causing a delayed increase in rotarod performance in both genotypes (Fig. 4e). Reference: Acta Neuropathol Commun. 2017 Mar 14;5(1):22. https://pubmed.ncbi.nlm.nih.gov/28292328/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| Water | 4.86 | 10.01 |
The following data is based on the product molecular weight 485.493 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Longo F, Mercatelli D, Novello S, Arcuri L, Brugnoli A, Vincenzi F, Russo I, Berti G, Mabrouk OS, Kennedy RT, Shimshek DR, Varani K, Bubacco L, Greggio E, Morari M. Age-dependent dopamine transporter dysfunction and Serine129 phospho-α-synuclein overload in G2019S LRRK2 mice. Acta Neuropathol Commun. 2017 Mar 14;5(1):22. doi: 10.1186/s40478-017-0426-8. PMID: 28292328; PMCID: PMC5351259. 2. Li C, Dabrowska J, Hazra R, Rainnie DG. Synergistic activation of dopamine D1 and TrkB receptors mediate gain control of synaptic plasticity in the basolateral amygdala. PLoS One. 2011;6(10):e26065. doi: 10.1371/journal.pone.0026065. Epub 2011 Oct 14. PMID: 22022509; PMCID: PMC3193533. |
| In vitro protocol: | TBD |
| In vivo protocol: | 1. Longo F, Mercatelli D, Novello S, Arcuri L, Brugnoli A, Vincenzi F, Russo I, Berti G, Mabrouk OS, Kennedy RT, Shimshek DR, Varani K, Bubacco L, Greggio E, Morari M. Age-dependent dopamine transporter dysfunction and Serine129 phospho-α-synuclein overload in G2019S LRRK2 mice. Acta Neuropathol Commun. 2017 Mar 14;5(1):22. doi: 10.1186/s40478-017-0426-8. PMID: 28292328; PMCID: PMC5351259. 2. Li C, Dabrowska J, Hazra R, Rainnie DG. Synergistic activation of dopamine D1 and TrkB receptors mediate gain control of synaptic plasticity in the basolateral amygdala. PLoS One. 2011;6(10):e26065. doi: 10.1371/journal.pone.0026065. Epub 2011 Oct 14. PMID: 22022509; PMCID: PMC3193533. |
1. Bonnet JJ, Protais P, Chagraoui A, Costentin J. High-affinity [3H]GBR 12783 binding to a specific site associated with the neuronal dopamine uptake complex in the central nervous system. Eur J Pharmacol. 1986;126(3):211-222. doi:10.1016/0014-2999(86)90050-6
2. Duterte-Boucher D, Kamenka JM, Costentin J. Comparison of the effects of three indirect dopamine agonists, GK 13, GBR 12783 and dexamphetamine on behavioural tests involving central catecholaminergic transmissions. Psychopharmacology (Berl). 1990;101(3):344-353. doi:10.1007/BF02244052
3. Bonnet JJ, Costentin J. GBR 12783, a potent and selective inhibitor of dopamine uptake: biochemical studies in vivo and ex vivo. Eur J Pharmacol. 1986;121(2):199-209. doi:10.1016/0014-2999(86)90491-7
