1H-3-Benzazepine-7,8-diol,6-chloro-2,3,4,5-tetrahydro-1-phenyl-3-(2-propen-1-yl)-, hydrobromide (1:1) - CAS 74115-01-8
Catalog number: 74115-01-8
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C19H21Cl NO2Br
Molecular Weight:
410.74
COA:
Inquire
Targets:
Dopamine Receptor
Description:
1H-3-Benzazepine-7,8-diol,6-chloro-2,3,4,5-tetrahydro-1-phenyl-3-(2-propen-1-yl)-, hydrobromide (1:1) is a synthetic compound belongs to the benzazepine class . It acts as a D1/D5 receptor full agonist. It produces characteristic anorectic effects, hyperactivity and self-administration in animals, which is similar to but not identical with dopaminergic stimulants such as amphetamine. It could increase renal blood flow in animal models and promote contralateral rotation in rats with unilateral lesions of the substantia nigra. It also could augment GABAB inhibitory post-synaptic potentials in ventral tegmental area in brain slices. It also acts as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen. In vivo, the acute injection of SKF-82958 would induce PPD, SP and PPE mRNA expression in the intact rat striatum.
Purity:
98%
Appearance:
White to off-white Solid
Synonyms:
6-Chloro-2,3,4,5-Tetrahydro-1-Phenyl-3-(2-Propen-1-Yl)-1H-3-Benzazepine-7,8-Diol Hydrobromide (1:1);SKF-82958 hydrobromide;(±)-SKF 82958 hydrobromide;Chloro-APB hydrobromide;(+/-)-6-Chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine HBr
Solubility:
H2O:< 6 mg/mL
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
1H-3-Benzazepine-7,8-diol,6-chloro-2,3,4,5-tetrahydro-1-phenyl-3-(2-propen-1-yl)-, hydrobromide (1:1) produces characteristic anorectic effects, hyperactivity and self-administration in animals. It could increase renal blood flow in animal models and promote contralateral rotation in rats with unilateral lesions of the substantia nigra. It also could augment GABAB inhibitory post-synaptic potentials in ventral tegmental area in brain slices. It also acts as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligram to gram
InChIKey:
WLXGFAVTAAQOFH-UHFFFAOYSA-N
InChI:
InChI=1S/C19H20ClNO2.BrH/c1-2-9-21-10-8-14-15(11-17(22)19(23)18(14)20)16(12-21)13-6-4-3-5-7-13;/h2-7,11,16,22-23H,1,8-10,12H2;1H
Canonical SMILES:
C=CCN1CCC2=C(C(=C(C=C2C(C1)C3=CC=CC=C3)O)O)Cl.Br
1.Prostaglandin E receptor EP1 forms a complex with dopamine D1 receptor and directs D1-induced cAMP production to adenylyl cyclase 7 through mobilizing G(βγ) subunits in human embryonic kidney 293T cells.
Ehrlich AT1, Furuyashiki T, Kitaoka S, Kakizuka A, Narumiya S. Mol Pharmacol. 2013 Sep;84(3):476-86. doi: 10.1124/mol.113.087288. Epub 2013 Jul 10.
The mechanism underlying the crosstalk between multiple G protein-coupled receptors remains poorly understood. We previously reported that prostaglandin E receptor EP1 facilitates dopamine D1 receptor signaling in striatal slices and promotes behavioral responses induced by D1 receptor agonists. Here, using human embryonic kidney (HEK)-293T cells expressing D1 and EP1, we have analyzed the mechanism underlying EP1-mediated facilitation of D1 receptor signaling. Fluorescent immunostaining showed that EP1 and D1 receptors are partly colocalized in the cells, and coprecipitation experiments revealed a molecular complex of EP1 and D1 receptors. Treatment of the cells with 17S,17,20-dimethyl-2,5-ethano-6-oxo-PGE₁ (ONO-DI-004), an EP1-selective agonist, enhanced cAMP production induced by D1 agonists (±)-6-chloro-2,3,4,5-tetrahydro-1-phenyl-1H-3-benzazepine hydrobromide (SKF-81297) and 6-chloro-2,3,4,5-tetrahydro-1-(3-methylphenyl)-3-(2-propenyl)-1H-3-benzazepine-7,8-diol hydrobromide (SKF-83822).
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