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MedKoo Cat#: 318193 | Name: Mesoridazine Besylate

Description:

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

Mesoridazine besylate is a phenothiazine dopamine receptor anatagonist. Mesoridazine besylate is described to demonstrate inhibition for D2DR and D4DR. It has a high affinity for dopamine D4 receptor. Mesoridazine besylate is an antipsychotic agent.

Chemical Structure

Mesoridazine Besylate
CAS#32672-69-8 (besylate)

Theoretical Analysis

MedKoo Cat#: 318193

Name: Mesoridazine Besylate

CAS#: 32672-69-8 (besylate)

Chemical Formula: C27H32N2O4S3

Exact Mass: 0.0000

Molecular Weight: 544.74

Elemental Analysis: C, 59.53; H, 5.92; N, 5.14; O, 11.75; S, 17.66

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Related CAS #
5588-33-0 (free base) 32672-69-8 (besylate) 59884-26-3 (HCl)
Synonym
Mesoridazine Besylate; Mesoridazine benzenesulfonate; NC 123; CHEBI:6781; C21H26N2OS2.C6H6O3S; PL054141; SAM001247051; SMR000449304; D00795;
IUPAC/Chemical Name
10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylsulfinyl)-10H-phenothiazine benzenesulfonate
InChi Key
CRJHBCPQHRVYBS-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H26N2OS2.C6H6O3S/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(26(2)24)15-19(21)23;7-10(8,9)6-4-2-1-3-5-6/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3;1-5H,(H,7,8,9)
SMILES Code
CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)C.C1=CC=C(C=C1)S(=O)(=O)O
Appearance
Yellow 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
Soluble in DMSO, not in water
Shelf Life
>3 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:
Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent.
In vitro activity:
Mesoridazine blocked HERG currents in a concentration-dependent manner (IC50 550 nM at 0 mV); block increased significantly over the voltage range where HERG activates and saturated at voltages eliciting maximal HERG channel activation. Reference: J Mol Cell Cardiol. 2004 Jan;36(1):151-60. https://pubmed.ncbi.nlm.nih.gov/14734057/
In vivo activity:
Using a subcutaneous injection model in rats, this study tested the cutaneous analgesic effects of six phenothiazine-type antipsychotics (mesoridazine, promazine, chlorpromazine, fluphenazine, perphenazine and triflupromazine) at a dose of 0.6 mumol, and compared them with those of bupivacaine and lidocaine. Mesoridazine had a longer duration of action than bupivacaine (p<0.001). In terms of ED(50) values, mesoridazine was more potent and longer-acting than bupivacaine and lidocaine (p<0.01 for each comparison). Reference: Acta Anaesthesiol Taiwan. 2010 Mar;48(1):3-7. https://pubmed.ncbi.nlm.nih.gov/20434106/

Preparing Stock Solutions

The following data is based on the product molecular weight 544.74 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.

Recalculate based on batch purity %
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. Su Z, Martin R, Cox BF, Gintant G. Mesoridazine: an open-channel blocker of human ether-a-go-go-related gene K+ channel. J Mol Cell Cardiol. 2004 Jan;36(1):151-60. doi: 10.1016/j.yjmcc.2003.10.017. PMID: 14734057. 2. Liu KS, Chen YW, Aljuffali IA, Chang CW, Wang JJ, Fang JY. Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment. Eur J Pharm Biopharm. 2016 Aug;105:59-68. doi: 10.1016/j.ejpb.2016.05.025. Epub 2016 May 31. PMID: 27260201. 3. Chen YW, Chu CC, Chu KS, Shieh JP, Chien CC, Wang JJ, Kao CH. Phenothiazine-type antipsychotics elicit cutaneous analgesia in rats. Acta Anaesthesiol Taiwan. 2010 Mar;48(1):3-7. doi: 10.1016/S1875-4597(10)60002-1. PMID: 20434106.
In vitro protocol:
1. Su Z, Martin R, Cox BF, Gintant G. Mesoridazine: an open-channel blocker of human ether-a-go-go-related gene K+ channel. J Mol Cell Cardiol. 2004 Jan;36(1):151-60. doi: 10.1016/j.yjmcc.2003.10.017. PMID: 14734057.
In vivo protocol:
1. Liu KS, Chen YW, Aljuffali IA, Chang CW, Wang JJ, Fang JY. Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment. Eur J Pharm Biopharm. 2016 Aug;105:59-68. doi: 10.1016/j.ejpb.2016.05.025. Epub 2016 May 31. PMID: 27260201. 2. Chen YW, Chu CC, Chu KS, Shieh JP, Chien CC, Wang JJ, Kao CH. Phenothiazine-type antipsychotics elicit cutaneous analgesia in rats. Acta Anaesthesiol Taiwan. 2010 Mar;48(1):3-7. doi: 10.1016/S1875-4597(10)60002-1. PMID: 20434106.
1: Morrow RJ, Millership JS, Collier PS. Diastereotopic analysis of mesoridazine besylate (Serentil). Chirality. 2004 Oct;16(8):534-40. PubMed PMID: 15290689. 2: Shader RI. Sexual dysfunction associated with mesoridazine besylate (serentil). Psychopharmacologia. 1972;27(3):293-4. PubMed PMID: 4674517. 3: Salih IS, Thanacoody RH, McKay GA, Thomas SH. Comparison of the effects of thioridazine and mesoridazine on the QT interval in healthy adults after single oral doses. Clin Pharmacol Ther. 2007 Nov;82(5):548-54. Epub 2007 Apr 4. PubMed PMID: 17410120. 4: Aguilar SJ. An open study of mesoridazine (Serentil) in chronic schizophrenics. Dis Nerv Syst. 1975 Sep;36(9):484-9. PubMed PMID: 1175465. 5: Niemann JT, Stapczynski JS, Rothstein RJ, Laks MM. Cardiac conduction and rhythm disturbances following suicidal ingestion of mesoridazine. Ann Emerg Med. 1981 Nov;10(11):585-8. PubMed PMID: 7316263. 6: Walker ST. Liquid chromatographic determination of organic nitrogenous bases in dosage forms: a progress report. J Assoc Off Anal Chem. 1985 May-Jun;68(3):539-42. PubMed PMID: 4019383. 7: Theesen KA, Wilson JE, Newton DW, Ueda CT. Compatibility of lithium citrate syrup with 10 neuroleptic solutions. Am J Hosp Pharm. 1981 Nov;38(11):1750-3. PubMed PMID: 6118064.

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CD12681

CD12681