SCH 23390 maleate | CAS#87134-87-0 | dopamine receptor antagonist

SCH 23390 maleate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526322

CAS#: 87134-87-0 (maleate)

Description: SCH 23390 is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). SCH 23390 is also an agonist at 5-HT1C and 5-HT2C receptors in vitro (Ki values are 6.3 nM and 9.3 nM respectively).

Chemical Structure

SCH 23390 maleate

CAS# 87134-87-0 (maleate)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526322
Name: SCH 23390 maleate
CAS#: 87134-87-0 (maleate)
Chemical Formula: C21H22ClNO5
Exact Mass: 0.00
Molecular Weight: 403.860
Elemental Analysis: C, 62.46; H, 5.49; Cl, 8.78; N, 3.47; O, 19.81

Price and Availability

Size	Price	Availability	Quantity
50mg	USD 650
100mg	USD 1050
200mg	USD 1750
500mg	USD 2450
1g	USD 3450
2g	USD 5450
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 125941-87-9 (HCl) 87075-17-0 (free base) 87134-87-0 (maleate)

Synonym: SCH-23390; SCH23390; SCH 23390; SCH-23390 maleate;

IUPAC/Chemical Name: (R)-8-chloro-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol maleate

InChi Key: FGHVSEXHEAUJBT-HFNHQGOYSA-N

InChi Code: InChI=1S/C17H18ClNO.C4H4O4/c1-19-8-7-13-9-16(18)17(20)10-14(13)15(11-19)12-5-3-2-4-6-12;5-3(6)1-2-4(7)8/h2-6,9-10,15,20H,7-8,11H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t15-;/m1./s1

SMILES Code: OC1=C(Cl)C=C2CCN(C)C[C@H](C3=CC=CC=C3)C2=C1.O=C(O)/C=C\C(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	SCH 23390 maleate is a dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH 23390 maleate is a human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH 23390 maleate inhibits GIRK channels with an IC50 of 268 nM.
In vitro activity:	In this study, SCH 23390 was discovered to inhibit GIRK channels, independent of receptor activation. The inhibition is selective, affecting GIRK currents induced by somatostatin or D3 dopamine receptors. SCH 23390 can depolarize membrane potential and induce action potentials in cells. Reference: Mol Pharmacol. 2002 Jul;62(1):119-26. https://pubmed.ncbi.nlm.nih.gov/12065762/
In vivo activity:	SCH 23390 may have use in addiction treatment research. In a saccharin seeking rat model, systemic SCH 23390 injections reduced saccharin seeking and reduced saccharin seeking persistence. Reference: Appetite. 2016 Oct 1;105:8-13. https://pubmed.ncbi.nlm.nih.gov/27179937/

Preparing Stock Solutions

The following data is based on the product molecular weight 403.86 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Kuzhikandathil EV, Oxford GS. 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. 2002 Jul;62(1):119-26. doi: 10.1124/mol.62.1.119. PMID: 12065762. 2. Millan MJ, Newman-Tancredi A, Quentric Y, Cussac D. The "selective" dopamine D1 receptor antagonist, SCH23390, is a potent and high efficacy agonist at cloned human serotonin2C receptors. Psychopharmacology (Berl). 2001 Jun;156(1):58-62. doi: 10.1007/s002130100742. PMID: 11465634. 3. Japarin RA, Harun N, Hassan Z, Müller CP. The dopamine D1 receptor antagonist SCH-23390 blocks the acquisition, but not expression of mitragynine-induced conditioned place preference in rats. Behav Brain Res. 2023 Sep 13;453:114638. doi: 10.1016/j.bbr.2023.114638. Epub 2023 Aug 22. PMID: 37619769. 4. Aoyama K, Barnes J, Koerber J, Glueck E, Dorsey K, Eaton L, Grimm JW. Systemic injection of the DAD1 antagonist SCH 23390 reduces saccharin seeking in rats. Appetite. 2016 Oct 1;105:8-13. doi: 10.1016/j.appet.2016.05.008. Epub 2016 May 11. PMID: 27179937; PMCID: PMC4980176.
In vitro protocol:	1. Kuzhikandathil EV, Oxford GS. 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. 2002 Jul;62(1):119-26. doi: 10.1124/mol.62.1.119. PMID: 12065762. 2. Millan MJ, Newman-Tancredi A, Quentric Y, Cussac D. The "selective" dopamine D1 receptor antagonist, SCH23390, is a potent and high efficacy agonist at cloned human serotonin2C receptors. Psychopharmacology (Berl). 2001 Jun;156(1):58-62. doi: 10.1007/s002130100742. PMID: 11465634.
In vivo protocol:	1. Japarin RA, Harun N, Hassan Z, Müller CP. The dopamine D1 receptor antagonist SCH-23390 blocks the acquisition, but not expression of mitragynine-induced conditioned place preference in rats. Behav Brain Res. 2023 Sep 13;453:114638. doi: 10.1016/j.bbr.2023.114638. Epub 2023 Aug 22. PMID: 37619769. 2. Aoyama K, Barnes J, Koerber J, Glueck E, Dorsey K, Eaton L, Grimm JW. Systemic injection of the DAD1 antagonist SCH 23390 reduces saccharin seeking in rats. Appetite. 2016 Oct 1;105:8-13. doi: 10.1016/j.appet.2016.05.008. Epub 2016 May 11. PMID: 27179937; PMCID: PMC4980176.

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1: Dhir A, Kulkarni SK. Involvement of dopamine (DA)/serotonin (5-HT)/sigma (sigma) receptor modulation in mediating the antidepressant action of ropinirole hydrochloride, a D2/D3 dopamine receptor agonist. Brain Res Bull. 2007 Sep 14;74(1-3):58-65. PubMed PMID: 17683790.

2: Rao TS, Reid RT, Correa LD, Santori EM, Gardner MF, Sacaan AI, Lorrain D, Vernier JM. In vivo pharmacological characterization of (+/-)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride (SIB-1553A), a novel cholinergic ligand: microdialysis studies. Brain Res. 2003 Oct 3;986(1-2):71-81. PubMed PMID: 12965231.

3: Fleckenstein AE, Pögün S, Carroll FI, Kuhar MJ. Recovery of dopamine transporter binding and function after intrastriatal administration of the irreversible inhibitor RTI-76 [3 beta-(3p-chlorophenyl) tropan-2 beta-carboxylic acid p-isothiocyanatophenylethyl ester hydrochloride]. J Pharmacol Exp Ther. 1996 Oct;279(1):200-6. PubMed PMID: 8858994.

4: Cheetham SC, Kettle CJ, Martin KF, Heal DJ. D1 receptor binding in rat striatum: modification by various D1 and D2 antagonists, but not by sibutramine hydrochloride, antidepressants or treatments which enhance central dopaminergic function. J Neural Transm Gen Sect. 1995;102(1):35-46. PubMed PMID: 8785022.

5: Napoleone P, Cavallotti C, Ricci A, Amenta F. Dopexamine hydrochloride in the human kidney: localization, receptor binding and effect on 3'-5'-cyclic adenosine monophosphate generation. Nephron. 1993;65(3):385-91. PubMed PMID: 7904730.

6: Napoleone P, Ricci A, Ferrante F, Amenta F. Dopexamine hydrochloride in the human heart: receptor binding and effects on cAMP generation. Eur Heart J. 1992 Dec;13(12):1709-17. PubMed PMID: 1363232.

7: Paalzow GH. L-dopa induces opposing effects on pain in intact rats: (-)-sulpiride, SCH 23390 or alpha-methyl-DL-p-tyrosine methylester hydrochloride reveals profound hyperalgesia in large antinociceptive doses. J Pharmacol Exp Ther. 1992 Nov;263(2):470-9. PubMed PMID: 1432683.

8: Bass AS. Presynaptic effects of dopexamine hydrochloride in the canine kidney. Naunyn Schmiedebergs Arch Pharmacol. 1992 Jan;345(1):33-6. PubMed PMID: 1347154.

9: Amenta F, Ricci A, Napoleone P, Vyas SJ, Lokhandwala MF. Anatomical localization of the binding and functional characterization of responses to dopexamine hydrochloride in the rat mesenteric vasculature. Pharmacology. 1991;42(4):211-22. PubMed PMID: 1677201.

10: Vyas SJ, Apparsundaram S, Ricci A, Amenta F, Lokhandwala MF. Biochemical, autoradiographic and pharmacological evidence for the involvement of tubular DA-1 receptors in the natriuretic response to dopexamine hydrochloride. Naunyn Schmiedebergs Arch Pharmacol. 1991 Jan;343(1):21-30. PubMed PMID: 1674360.

11: Bass AS. Contrasting effects of dopexamine hydrochloride on electrolyte excretion in canine kidney. J Pharmacol Exp Ther. 1990 May;253(2):798-802. PubMed PMID: 1971021.

12: Chintala MS, Lokhandwala MF, Jandhyala BS. Protective effects of dopexamine hydrochloride in renal failure after acute haemorrhage in anaesthetized dogs. J Auton Pharmacol. 1990;10 Suppl 1:s95-102. PubMed PMID: 1965897.

13: Smith GW, Hall JC, Farmer JB, Simpson WT. The cardiovascular actions of dopexamine hydrochloride, an agonist at dopamine receptors and beta 2-adrenoceptors in the dog. J Pharm Pharmacol. 1987 Aug;39(8):636-41. PubMed PMID: 2888855.

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