GBR-12783 dihydrochloride
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MedKoo CAT#: 574707

CAS#: 67469-75-4

Description: GBR-12783 dihydrochloride is a Dopamine uptake inhibitor.


Chemical Structure

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GBR-12783 dihydrochloride
CAS# 67469-75-4

Theoretical Analysis

MedKoo Cat#: 574707
Name: GBR-12783 dihydrochloride
CAS#: 67469-75-4
Chemical Formula: C28H34Cl2N2O
Exact Mass: 0.00
Molecular Weight: 485.493
Elemental Analysis: C, 69.27; H, 7.06; Cl, 14.60; N, 5.77; O, 3.30

Price and Availability

Size Price Availability Quantity
10mg USD 275 2 Weeks
50mg USD 765 2 Weeks
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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

More Info:

Product Data:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Water 4.9 10.01

Preparing Stock Solutions

The following data is based on the product molecular weight 485.49 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.

Recalculate based on batch purity %
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.

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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