SCH 23390 hydrochloride

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Cat.No. 0925 - SCH 23390 hydrochloride | C17H18ClNO.HCl | CAS No. 125941-87-9
Description: Standard selective D1-like antagonist; also 5-HT2C and 5-HT1C agonist and Kir3 channel blocker
Alternative Names: (R)-(+)-SCH 23390 hydrochloride
Chemical Name: (R)-(+)-7-Chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (40)
Literature

Biological Activity

Potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). Also an agonist at 5-HT1C and 5-HT2C receptors in vitro (Ki values are 6.3 nM and 9.3 nM respectively). Blocks quinpirole-induced Kir3 (GIRK) currents (EC50 = 268 nM) independently of receptors.

Technical Data

M. Wt 324.24
Formula C17H18ClNO.HCl
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 125941-87-9
PubChem ID 11957535
InChI Key OYCAEWMSOPMASE-XFULWGLBSA-N
Smiles ClC1=C(O)C=C([C@](C3=CC=CC=C3)([H])C2)C(CCN2C)=C1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 32.42 100
ethanol 16.21 50
water 32.42 100mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 324.24. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.08 mL 15.42 mL 30.84 mL
5 mM 0.62 mL 3.08 mL 6.17 mL
10 mM 0.31 mL 1.54 mL 3.08 mL
50 mM 0.06 mL 0.31 mL 0.62 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Bourne et al (2001) SCH 23390: The first selective dopamine D1-like receptor antagonist. CNS Drug Rev. 7 399 PMID: 11830757

Briggs et al (1991) Activation of the 5-HT1C receptor expressed in Xenopus oocytes by the benzazepines SCH 23390 and SKF 38393. Br.J.Pharmacol. 104 1038 PMID: 1687364

Millan et al (2001) The "selective" dopamine D1 receptor antagonist, SCH23390, is a potent and high efficacy agonist against cloned human serotonin2C receptors. Psychopharmacology 156 58 PMID: 11465634

Kuzhikandathil and Oxford (2002) Classic D1 dopamine receptor antagonist R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (SCH23390) directly inhibits G protein-coupled inwardly rectifying potassium channels. Mol.Pharmacol. 62 119 PMID: 12065762


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Keywords: 5-HT2C agonists potent D1-like antagonists selective Serotonin Receptors Dopamine D1 D5 dopaminergic SCH23390 hydrochloride (R)-(+)-SCH 23390 hydrochloride D1 and D5 Receptors

40 Citations for SCH 23390 hydrochloride

Citations are publications that use Tocris products. Selected citations for SCH 23390 hydrochloride include:

Prado et al (2012) Stimulation of dopamine receptor D5 expressed on dendritic cells potentiates Th17-mediated immunity. Psychopharmacology (Berl) 188 3062 PMID: 22379034

Huang et al (2012) SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes. Neuroscience 7 e49954 PMID: 23185493

Shin et al (2011) Exposure to extremely low frequency magnetic fields induces fos-related antigen-immunoreactivity via activation of dopaminergic d1 receptor. Hum Mol Genet 20 130 PMID: 22110371

Krishnan et al (2010) Dopamine receptor mechanisms mediate corticotropin-releasing factor-induced long-term potentiation in the rat amygdala following cocaine withdrawal. Eur J Neurosci 31 1027 PMID: 20377617

Raghuraman et al (2010) Post-translational modification of glutamic acid decarboxylase 67 by intermittent hypoxia: evidence for the involvement of dopamine D1 receptor signaling. J Neurochem 115 1568 PMID: 20969567

Xu et al (2010) Amphetamine modulation of long-term potentiation in the prefrontal cortex: dose dependency, monoaminergic contributions, and paradoxical rescue in hyperdopaminergic mutant. Exp Neurobiol 115 1643 PMID: 20969573

Goffin et al (2010) Dopamine-dependent tuning of striatal inhibitory synaptogenesis. J Neurosci 30 2935 PMID: 20181591

Deng et al (2010) MeCP2 in the nucleus accumbens contributes to neural and behavioral responses to psychostimulants. J Ginseng Res 13 1128 PMID: 20711186

Schwendt and McGinty (2010) Amphetamine up-regulates activator of G-protein signaling 1 mRNA and protein levels in rat frontal cortex: the role of dopamine and glucocorticoid receptors. J Neurosci 168 96 PMID: 20298760

Chuhma et al (2009) Dopamine neuron glutamate cotransmission: frequency-dependent modulation in the mesoventromedial projection. Neuroscience 164 1068 PMID: 19729052

Xu et al (2009) Hyperdopaminergic tone erodes prefrontal long-term potential via a D2 receptor-operated protein phosphatase gate. J Immunol 29 14086 PMID: 19906957

Costa et al (2008) Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition. J Neurosci 28 8040 PMID: 18685029

Kash et al (2008) Dopamine enhances fast excitatory synaptic transmission in the extended amygdala by a CRF-R1-dependent process. J Neurochem 28 13856 PMID: 19091975

Witkovsky et al (2007) Cellular localization and function of DARPP-32 in the rodent retina. Eur J Neurosci 25 3233 PMID: 17552992

Clancy et al (2007) Coregulation of natively expressed pertussis toxin-sensitive muscarinic receptors with G-protein-activated potassium channels. PLoS One 27 6388 PMID: 17567799

Rao et al (2007) Prolonged wakefulness induces experience-dependent synaptic plasticity in mouse hypocretin/orexin neurons. J Neurosci 117 4022 PMID: 18060037

Meredith et al (2006) Dopamine targets cycling B cells independent of receptors/transporter for oxidative attack: Implications for non-Hodgkin's lymphoma. Proc Natl Acad Sci U S A 103 13485 PMID: 16938864

Scheggi (2017) Fasting biases μ-opioid receptors toward β-arrestin2 dependent signaling in the accumbens shell. Neuroscience 352 19 PMID: 28391016

Kasaharaa et al (2016) The σ1 receptor regulates accumulation of GM1 ganglioside-enriched autophagosomes in astrocytes Neuroscience 340 176 PMID: 27815022

Mamaligas et al (2016) Nicotinic and opioid receptor regulation of striatal dopamine D2-receptor mediated transmission Scientific Reports 6 37834 PMID: 27886263

Brzosko et al (2015) Retroactive modulation of spike timing-dependent plasticity by dopamine. Elife 4 PMID: 26516682

Tozzi et al (2015) Endogenous 17β-estradiol is required for activity-dependent long-term potentiation in the striatum: interaction with the dopaminergic system. Front Cell Neurosci 9 192 PMID: 26074768

Hao et al (2015) L-Stepholidine rescues memory deficit and synaptic plasticity in models of Alzheimer's disease via activating dopamine D1 receptor/PKA signaling pathway. Cell Death Dis 6 e1965 PMID: 26539912

Meunier et al (2015) Effect of dopaminergic D1 receptors on plasticity is dependent of serotoninergic 5-HT1A receptors in L5-pyramidal neurons of the prefrontal cortex. PLoS One 10 e0120286 PMID: 25775449

Kim et al (2015) Spinal dopaminergic projections control the transition to pathological pain plasticity via a D1/D5-mediated mechanism. J Neurosci 35 6307 PMID: 25904784

Li et al (2015) Incubation of methamphetamine craving is associated with selective increases in expression of Bdnf and trkb, glutamate receptors, and epigenetic enzymes in cue-activated fos-expressing dorsal striatal neurons. Learn Mem 35 8232 PMID: 26019338

Savalli et al (2015) Regionally selective requirement for D1/D5 dopaminergic neurotransmission in the medial prefrontal cortex in object-in-place associative recognition memory. PLoS One 22 69 PMID: 25593292

Montalbano et al (2015) Pharmacological Characterization of 5-HT1A Autoreceptor-Coupled GIRK Channels in Rat Dorsal Raphe 5-HT Neurons. J Pharmacol Exp Ther 10 e0140369 PMID: 26460748

Conley et al (2015) Evaluation of AaDOP2 receptor antagonists reveals antidepressants and antipsychotics as novel lead molecules for control of the yellow fever mosquito, Aedes aegypti. PLoS One 352 53 PMID: 25332454

Rioult-Pedotti et al (2015) Dopamine Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation. PLoS One 10 e0124986 PMID: 25938462

Pezze et al (2015) Dopaminergic modulation of appetitive trace conditioning: the role of D1 receptors in medial prefrontal cortex. Behav Neurosci 232 2669 PMID: 25820982

Lee and Chirwa (2015) Blocking Dopaminergic Signaling Soon after Learning Impairs Memory Consolidation in Guinea Pigs. Nat Neurosci 10 e0135578 PMID: 26275140

Marchant and Kaganovsky (2015) A critical role of nucleus accumbens dopamine D1-family receptors in renewal of alcohol seeking after punishment-imposed abstinence. PLoS One 129 281 PMID: 25914922

Marcott et al (2014) Phasic dopamine release drives rapid activation of striatal D2-receptors. Neuron 84 164 PMID: 25242218

Ribeiro et al (2014) Metabotropic glutamate receptor 5 knockout promotes motor and biochemical alterations in a mouse model of Huntington's disease. J Neurosci 23 2030 PMID: 24282028

Zhao et al (2014) Korean Red Ginseng attenuates anxiety-like behavior during ethanol withdrawal in rats. Br J Pharmacol 38 256 PMID: 25379005

Fuenzalida et al (2014) Dopamine D1 and corticotrophin-releasing hormone type-2α receptors assemble into functionally interacting complexes in living cells. J Clin Invest 171 5650 PMID: 25073922

Jia et al (2013) Age-dependent regulation of synaptic connections by dopamine D2 receptors. Nat Neurosci 16 1627 PMID: 24121738

Zhang et al (2013) Sucrose produces withdrawal and dopamine-sensitive reinforcing effects in planarians. Physiol Behav 112-113 8 PMID: 23415661

Lisek et al (2012) Mephedrone ('bath salt') elicits conditioned place preference and dopamine-sensitive motor activation. Drug Alcohol Depend 126 257 PMID: 22652295


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