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G0544

Sigma-Aldrich

GR 103691

≥98% (HPLC), solid

Synonym(s):

4′-Acetyl-N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-[1,1′-biphenyl]-4-carboxamide

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About This Item

Empirical Formula (Hill Notation):
C30H35N3O3
CAS Number:
162408-66-4
Molecular Weight:
485.62
MDL number:
MFCD00936840
UNSPSC Code:
12352200
PubChem Substance ID:
24724488
NACRES:
NA.77

Assay

≥98% (HPLC)

form

solid

color

white

solubility

DMSO: soluble >5 mg/mL at 60 °C

originator

GlaxoSmithKline

storage temp.

2-8°C

SMILES string

COc1ccccc1N2CCN(CCCCNC(=O)c3ccc(cc3)-c4ccc(cc4)C(C)=O)CC2

InChI

1S/C30H35N3O3/c1-23(34)24-9-11-25(12-10-24)26-13-15-27(16-14-26)30(35)31-17-5-6-18-32-19-21-33(22-20-32)28-7-3-4-8-29(28)36-2/h3-4,7-16H,5-6,17-22H2,1-2H3,(H,31,35)

InChI key

JARNORYOPMINDY-UHFFFAOYSA-N

Gene Information

rat ... Htr1a(24473)

Application

GR 103691 has been used as a D3 receptor antagonist to test its:
  • inducing effect on prepulse inhibition (PPI)
  • suppressive effect of motor behavior in rats
  • inhibitory effect on chemotaxis in newly excysted juvenile C. sinensis (CsNEJs)

Biochem/physiol Actions

GR 103691 increases the monosynaptic “stretch” reflex (MSR) amplitude in mice by its potent D3 receptor antagonist functionality. It inhibits the PD 128,907 mediated γ-aminobutyric acid (GABA) release.
D3 dopamine receptor antagonist.

Features and Benefits

This compound is featured on the Dopamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

Sold for research purposes under agreement from Glaxo­Smith­Kline

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Roberto Frau et al.
Psychoneuroendocrinology, 63, 59-67 (2015-09-29)
Neurosteroids exert diverse modulatory actions on dopamine neurotransmission and signaling. We previously documented that the enzyme 5α-reductase, which catalyzes the main rate-limiting step in neurosteroid synthesis, is required for the behavioral responses of Sprague-Dawley rats to non-selective dopaminergic agonists, such
Refugio Cruz-Trujillo et al.
Neuropharmacology, 67, 370-378 (2012-12-15)
The firing rate of substantia nigra reticulata (SNr) neurons is modulated by GABA release from striatonigral and pallidonigral projections. This release is, in turn, modulated by dopamine acting on dopamine D1 receptors at striatonigral terminals and D4 receptors at pallidonigral
Shunyu Li et al.
PLoS neglected tropical diseases, 13(8), e0007573-e0007573 (2019-08-14)
The metacercariae of the Clonorchis sinensis liver fluke excyst in the duodenum of mammalian hosts, and the newly excysted juveniles (CsNEJs) migrate along the bile duct via bile chemotaxis. Cholic acid is a major component of bile that induces this
Suhail Kasim et al.
Developmental neuroscience, 28(6), 505-517 (2006-10-10)
In rodents, activation of L-type calcium channels with +/-BayK 8644 causes an unusual behavioral syndrome that includes dystonia and self-biting. Prior studies have linked both of these behaviors to dysfunction of dopaminergic transmission in the striatum. The current studies were
Stefan Clemens et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 24(50), 11337-11345 (2004-12-17)
Descending monoaminergic systems modulate spinal cord function, yet spinal dopaminergic actions are poorly understood. Using the in vitro lumbar cord, we studied the effects of dopamine and D2-like receptor ligands on spinal reflexes in wild-type (WT) and D3-receptor knock-out mice

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