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G0544

GR 103691

Name: GR 103691
Brand: SIGMA

≥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

Quality Level

100

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

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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The neurosteroidogenic enzyme 5α-reductase modulates the role of D1 dopamine receptors in rat sensorimotor gating.

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

Chemotactic migration of newly excysted juvenile Clonorchis sinensis is suppressed by neuro-antagonists.

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

D3 dopamine receptors interact with dopamine D1 but not D4 receptors in the GABAergic terminals of the SNr of the rat.

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

The role of dopamine receptors in the neurobehavioral syndrome provoked by activation of L-type calcium channels in rodents.

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

Conversion of the modulatory actions of dopamine on spinal reflexes from depression to facilitation in D3 receptor knock-out mice.

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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