GBR-12783 dihydrochloride | CAS# 67469-75-4 | Biochemical

MedKoo Cat#: 574707 | Name: GBR-12783 dihydrochloride

Featured

Description:

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

GBR-12783 dihydrochloride is a Dopamine uptake inhibitor.

Chemical Structure

GBR-12783 dihydrochloride

CAS#67469-75-4 (2HCl)

Theoretical Analysis

MedKoo Cat#: 574707

Name: GBR-12783 dihydrochloride

CAS#: 67469-75-4 (2HCl)

Chemical Formula: C28H34Cl2N2O

Exact Mass: 0.0000

Molecular Weight: 485.49

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 350.00	2 Weeks
50mg	USD 950.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

67469-57-2 (free base) 67469-75-4 (2HCl)

Synonym

GBR-12783 dihydrochloride; GBR-12783 2HCl; GBR-12783; GBR12783; GBR 12783; GBR 12921; GBR12921; GBR-12921

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

Product Data

Instruction

View handling instruction

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	mg/mL	mM
Solubility
	Water	4.9	10.01

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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. 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