MedKoo Cat#: 574706 | Name: GBR-12783
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GBR-12783 is a very potent and selective inhibitor of dopamine uptake.

Chemical Structure

GBR-12783
GBR-12783
CAS#67469-57-2 (free base)

Theoretical Analysis

MedKoo Cat#: 574706

Name: GBR-12783

CAS#: 67469-57-2 (free base)

Chemical Formula: C28H32N2O

Exact Mass: 412.2515

Molecular Weight: 412.58

Elemental Analysis: C, 81.51; H, 7.82; N, 6.79; O, 3.88

Price and Availability

Size Price Availability Quantity
25mg USD 350.00 2 Weeks
100mg USD 650.00 2 Weeks
1g USD 1,250.00 2 Weeks
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Synonym
GBR-12783; GBR12783; GBR 12783; GBR 12921; GBR12921; GBR-12921
IUPAC/Chemical Name
1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenyl-2-propen-1-yl)piperazine
InChi Key
XFBDGHFDKJITGC-JLHYYAGUSA-N
InChi Code
InChI=1S/C28H32N2O/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/b13-10+
SMILES Code
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 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/

Preparing Stock Solutions

The following data is based on the product molecular weight 412.58 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.
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