G0544
GR 103691
≥98% (HPLC), solid
别名:
4′-Acetyl-N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-[1,1′-biphenyl]-4-carboxamide
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关于此项目
经验公式（希尔记法）:
C30H35N3O3
化学文摘社编号:
分子量:
485.62
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI key
JARNORYOPMINDY-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
solid
color
white
solubility
DMSO: soluble >5 mg/mL at 60 °C
originator
GlaxoSmithKline
storage temp.
2-8°C
Quality Level
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
D3 dopamine receptor antagonist.
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.
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
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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
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
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
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
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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