Mianserin | CAS#24219-97-4

MedKoo Cat#: 318267 | Name: Mianserin

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Description:

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

Mianserin is a psychoactive drug of the tetracyclic antidepressant (TeCA) therapeutic family. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA) and has antidepressant, anxiolytic (anti-anxiety), hypnotic (sedating), antiemetic (nausea and vomiting-attenuating), orexigenic (appetite-stimulating), and antihistamine effects.

Chemical Structure

Mianserin

CAS#24219-97-4 (free base)

Theoretical Analysis

MedKoo Cat#: 318267

Name: Mianserin

CAS#: 24219-97-4 (free base)

Chemical Formula: C18H20N2

Exact Mass: 264.1626

Molecular Weight: 264.36

Elemental Analysis: C, 81.78; H, 7.63; N, 10.60

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100mg	USD 450.00	Back order

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Related CAS #

24219-97-4 (free base) 21535-47-7 (HCl) 51152-88-6 ((S)-isomer)

Synonym

Mianserin, Depnon, Lantanon, Lerivon, Lumin, Norval, Tolvon; Mianserine;

IUPAC/Chemical Name

2-methyl-1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine

InChi Key

UEQUQVLFIPOEMF-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H20N2/c1-19-10-11-20-17-9-5-3-7-15(17)12-14-6-2-4-8-16(14)18(20)13-19/h2-9,18H,10-13H2,1H3

SMILES Code

CN1CCN2C(C1)C3=CC=CC=C3CC4=CC=CC=C42

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

Soluble in DMSO, not in water

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:

Mianserin is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.

In vitro activity:

Effects of mianserin were examined in CHO cells transfected with human opioid receptors, C6 glioma cells and rat brain membranes by the use of radioligand binding and functional assays including the stimulation of [(35)S]GTPγS binding and MAPK phosphorylation. Mianserin displayed 12- and 18-fold higher affinity for κ- than µ- and δ-opioid receptors respectively. In [(35)S]GTPγS assays, mianserin selectively activated κ-opioid receptors. Mianserin and mirtazapine increased ERK1/2 phosphorylation in CHO cells expressing κ-opioid receptors and C6 cells, and these effects were antagonized by nor-BNI. Reference: Br J Pharmacol. 2012 Nov;167(6):1329-41. https://pubmed.ncbi.nlm.nih.gov/22708686/

In vivo activity:

This study used various experimental pain methods to investigate the effects of subacute mianserin administration on diabetes-induced neuropathic pain in rats. At 30 and 45 mg/kg, mianserin effectively improved mechanical and thermal hyperalgesia occurring in connection with diabetic neuropathy. Subacute administration of mianserin also reduced diabetes-associated mechanical and thermal allodynia. The ability of mianserin to reduce diabetic neuropathic pain was comparable to that of pregabalin (10mg/kg). These results suggest that the beneficial effect of mianserin on diabetic neuropathic pain is mediated through an increase in catecholamine levels in the synaptic cleft as well as through interactions with both subtypes of adrenoceptors and opioid receptors. Reference: Eur J Pharmacol. 2015 Jun 5;756:92-106. https://pubmed.ncbi.nlm.nih.gov/25771454/

	Solvent	mg/mL	mM	comments
Solubility
	Soluble in DMSO, not in water	0.0	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 264.36 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. Okura T, Ohkawara B, Takegami Y, Ito M, Masuda A, Seki T, Ishiguro N, Ohno K. Mianserin suppresses R-spondin 2-induced activation of Wnt/β-catenin signaling in chondrocytes and prevents cartilage degradation in a rat model of osteoarthritis. Sci Rep. 2019 Feb 26;9(1):2808. doi: 10.1038/s41598-019-39393-x. Erratum in: Sci Rep. 2020 Feb 14;10(1):2995. PMID: 30808932; PMCID: PMC6391487. 2. Olianas MC, Dedoni S, Onali P. The atypical antidepressant mianserin exhibits agonist activity at κ-opioid receptors. Br J Pharmacol. 2012 Nov;167(6):1329-41. doi: 10.1111/j.1476-5381.2012.02078.x. PMID: 22708686; PMCID: PMC3504997. 3. Üçel Uİ, Can ÖD, Demir Özkay Ü, Öztürk Y. Antihyperalgesic and antiallodynic effects of mianserin on diabetic neuropathic pain: a study on mechanism of action. Eur J Pharmacol. 2015 Jun 5;756:92-106. doi: 10.1016/j.ejphar.2015.02.048. Epub 2015 Mar 11. PMID: 25771454. 4. Manikowska K, Mikołajczyk M, Mikołajczak PŁ, Bobkiewicz-Kozłowska T. The influence of mianserin on TNF-α, IL-6 and IL-10 serum levels in rats under chronic mild stress. Pharmacol Rep. 2014 Feb;66(1):22-7. doi: 10.1016/j.pharep.2013.06.003. Epub 2014 Feb 4. PMID: 24905302.

In vitro protocol:

In vivo protocol:

1. Üçel Uİ, Can ÖD, Demir Özkay Ü, Öztürk Y. Antihyperalgesic and antiallodynic effects of mianserin on diabetic neuropathic pain: a study on mechanism of action. Eur J Pharmacol. 2015 Jun 5;756:92-106. doi: 10.1016/j.ejphar.2015.02.048. Epub 2015 Mar 11. PMID: 25771454. 2. Manikowska K, Mikołajczyk M, Mikołajczak PŁ, Bobkiewicz-Kozłowska T. The influence of mianserin on TNF-α, IL-6 and IL-10 serum levels in rats under chronic mild stress. Pharmacol Rep. 2014 Feb;66(1):22-7. doi: 10.1016/j.pharep.2013.06.003. Epub 2014 Feb 4. PMID: 24905302.

1: Isabelle le BL, Clarot F, Vaz E, Goullé JP, Proust B. Disopyramide and mianserin intoxication: a unique fatal case--review of the literature. J Forensic Sci. 2014 May;59(3):850-3. doi: 10.1111/1556-4029.12392. Epub 2014 Feb 6. Review. PubMed PMID: 24502246. 2: Poyurovsky M, Schneidman M, Weizman A. Successful treatment of fluoxetine-induced dystonia with low-dose mianserin. Mov Disord. 1997 Nov;12(6):1102-5. Review. PubMed PMID: 9399252. 3: Leinonen E, Koponen H, Lepola U. Serum mianserin and ageing. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Sep;18(5):833-45. Review. PubMed PMID: 7972855. 4: Tiraboschi P. [Mianserin]. Medicina (Firenze). 1988 Jul-Sep;8(3):351-3. Review. Italian. PubMed PMID: 3068469. 5: Wakeling A. Efficacy and side effects of mianserin, a tetracyclic antidepressant. Postgrad Med J. 1983 Apr;59(690):229-31. Review. PubMed PMID: 6346303; PubMed Central PMCID: PMC2417496. 6: Pinder RM, Fink M. Mianserin. Mod Probl Pharmacopsychiatry. 1982;18:70-101. Review. PubMed PMID: 7048075. 7: Cassano GB, Conti L, Dell'Osso L, Massimetti G. Four new atypical antidepressants (trazodone, mianserin, nomifensine, caroxazone): results of controlled trials. Adv Biochem Psychopharmacol. 1982;32:125-39. Review. PubMed PMID: 7046361. 8: Leonard BE. On the mode of action of mianserin. Adv Biochem Psychopharmacol. 1982;31:301-19. Review. PubMed PMID: 6282060. 9: Haine SE, Miljoen HP, Blankoff I, Vrints CJ. Mianserin and ventricular tachycardia: case report and review of the literature. Cardiology. 2006;106(4):195-8. Epub 2006 May 3. Review. PubMed PMID: 16675906. 10: Rotzinger S, Bourin M, Akimoto Y, Coutts RT, Baker GB. Metabolism of some "second"- and "fourth"-generation antidepressants: iprindole, viloxazine, bupropion, mianserin, maprotiline, trazodone, nefazodone, and venlafaxine. Cell Mol Neurobiol. 1999 Aug;19(4):427-42. Review. PubMed PMID: 10379419. 11: Demling J. [Mianserin: pharmacology and clinical aspects of an effective antidepressive agents]. Fortschr Med. 1993 Nov 10;111(31):497-500. Review. German. PubMed PMID: 8276338. 12: Mianserin 10 years on. Drug Ther Bull. 1988 Mar 7;26(5):17-8. Review. PubMed PMID: 3286177. 13: Boschmans SA, Perkin MF, Terblanche SE. Antidepressant drugs: imipramine, mianserin and trazodone. Comp Biochem Physiol C. 1987;86(2):225-32. Review. PubMed PMID: 2882911. 14: Chaplin S. Bone marrow depression due to mianserin, phenylbutazone, oxyphenbutazone, and chloramphenicol--Part II. Adverse Drug React Acute Poisoning Rev. 1986 Autumn;5(3):181-96. Review. PubMed PMID: 3538824. 15: Chaplin S. Bone marrow depression due to mianserin, phenylbutazone, oxyphenbutazone, and chloramphenicol--Part I. Adverse Drug React Acute Poisoning Rev. 1986 Summer;5(2):97-136. Review. Erratum in: Adverse Drug React Acute Poisoning Rev 1986 Winter;5(4):233. PubMed PMID: 3529881. 16: Lingjaerde O. From clomipramine to mianserin: therapeutic relevance of interactions with serotonin uptake and storage, as studied in the blood platelet model. Acta Psychiatr Scand Suppl. 1985;320:10-9. Review. PubMed PMID: 3901671. 17: Pinder RM. Adrenoreceptor interactions of the enantiomers and metabolites of mianserin: are they responsible for the antidepressant effect? Acta Psychiatr Scand Suppl. 1985;320:1-9. Review. PubMed PMID: 2996305. 18: De Ridder JJ. Mianserin: result of a decade of antidepressant research. Pharm Weekbl Sci. 1982 Oct 22;4(5):139-45. Review. PubMed PMID: 6128715. 19: Montgomery SA. Maprotiline, nomifensine, mianserin, zimelidine: a review of antidepressant efficacy in in-patients. Neuropharmacology. 1980 Dec;19(12):1185-90. Review. PubMed PMID: 6449677. 20: Brogden RN, Heel RC, Speight TM, Avery GS. Mianserin: a review of its pharmacological properties and therapeutic efficacy in depressive illness. Drugs. 1978 Oct;16(4):273-301. Review. PubMed PMID: 359311.

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MI-538

MedKoo CAT#: 407252

CAS#: 1857417-10-7

25mg / USD -2.00