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24219-97-4

24219-97-4 structure

Name: Mianserin
Chemical Name: mianserin
CAS Number: 24219-97-4
Molecular Formula: C₁₈H₂₀N₂
Molecular Weight: 264.36500
Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
Create Date: 2018-06-30 09:29:23
Modify Date: 2024-01-03 18:02:56
Mianserin is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.Target: H1 receptorMianserin 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. It is not approved for use in the US, but its analogue, mirtazapine, is. Mianserin was the first antidepressant to reach the UK market that was less dangerous than the tricyclic antidepressants in overdose.Mianserin is an antagonist/inverse agonist of the H1, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, and α2-adrenergic receptors, and also inhibits the reuptake of norepinephrine. As a high affinity H1 receptor inverse agonist, mianserin has strong antihistamine effects (sedation, weight gain, etc.). Contrarily, it has negligible affinity for the mACh receptors, and thus lacks any anticholinergic properties. It was recently found to be a potent kappa opioid receptor agonist. In addition, mianserin also appears to be a potent antagonist of the neuronal octopamine receptor. What implications this may have on mood are currently unknown, however octopamine has been implicated in the regulation of sleep, appetite and insulin production and therefore may theoretically contribute to the overall side effect profile of mianserin.

Name	mianserin
Synonyms	[3H]-(+/-)-Mianserin Org-4360 (R)-Mianserine Org-5859 MIANSERIN Dibenzoc,fpyrazino1,2-aazepine,1,2,3,4,10,14b-hexahydro-2-methyl (S)-Mianserine 2-methyl-1,2,3,4,10,14b-hexahydro-dibenzo[c,f]pyrazino[1,2-a]azepine

Description	Mianserin is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.Target: H1 receptorMianserin 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. It is not approved for use in the US, but its analogue, mirtazapine, is. Mianserin was the first antidepressant to reach the UK market that was less dangerous than the tricyclic antidepressants in overdose.Mianserin is an antagonist/inverse agonist of the H1, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, and α2-adrenergic receptors, and also inhibits the reuptake of norepinephrine. As a high affinity H1 receptor inverse agonist, mianserin has strong antihistamine effects (sedation, weight gain, etc.). Contrarily, it has negligible affinity for the mACh receptors, and thus lacks any anticholinergic properties. It was recently found to be a potent kappa opioid receptor agonist. In addition, mianserin also appears to be a potent antagonist of the neuronal octopamine receptor. What implications this may have on mood are currently unknown, however octopamine has been implicated in the regulation of sleep, appetite and insulin production and therefore may theoretically contribute to the overall side effect profile of mianserin.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Histamine Receptor Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Neurological Disease
References	[1]. Olianas MC, et al. The atypical antidepressant mianserin exhibits agonist activity at κ-opioid receptors. Br J Pharmacol. 2012 Nov;167(6):1329-41. [2]. Roeder T. High-affinity antagonists of the locust neuronal octopamine receptor. Eur J Pharmacol. 1990 Nov 27;191(2):221-4.

Density	1.18g/cm3
Boiling Point	411.3ºC at 760mmHg
Molecular Formula	C₁₈H₂₀N₂
Molecular Weight	264.36500
Flash Point	186.1ºC
Exact Mass	264.16300
PSA	6.48000
LogP	3.08680
Storage condition	2-8℃

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HP8778000

CHEMICAL NAME :: Dibenzo(c,f)pyrazino(1,2-a)azepine, 1,2,3,4,10,14b-hexahydro-2-methyl-

CAS REGISTRY NUMBER :: 24219-97-4

LAST UPDATED :: 199706

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C18-H20-N2

MOLECULAR WEIGHT :: 264.40

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 9 mg/kg/3W-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Cardiac - other changes

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 140,166,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 25 mg/kg/6W-I

TOXIC EFFECTS :: Blood - agranulocytosis

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 291,1375,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1200 ug/kg

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction) Cardiac - change in rate

REFERENCE :: HETOEA Human & Experimental Toxicology. (Macmillan Press Ltd., Brunel Road, Houndmills, Basingstoke, Hampshire, RG21 2XS, UK) V.9- 1990- Volume(issue)/page/year: 10,383,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 365 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DDREDK Drug Development Research. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 3,357,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 130 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: APPHAX Acta Poloniae Pharmaceutica. For English translation, see APPFAR. (Ars Polona, POB 1001, 00-680 Warsaw 1, Poland) V.1- 1937- Volume(issue)/page/year: 40,235,1983 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 65 mg/kg

SEX/DURATION :: female 8-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral

REFERENCE :: ATSUDG Archives of Toxicology, Supplement. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) No.1- 1978- Volume(issue)/page/year: 7,504,1984

RIDADR	UN 3249
Packaging Group	III
Hazard Class	6.1(b)
HS Code	2933990090

61337-89-1

~78%

24219-97-4

Literature: Sumitomo Chemical Company, Limited Patent: EP2135870 A1, 2009 ; Location in patent: Page/Page column 5-6 ;

21535-46-6

~87%

24219-97-4

Literature: Hulinska, Hana; Polivka, Zdenek; Jilek, Jiri; Sindelar, Karel; Holubek, Jiri; et al. Collection of Czechoslovak Chemical Communications, 1988 , vol. 53, # 8 p. 1820 - 1844

Precursor 1
61337-89-1
DownStream 4
57257-81-5 71936-92-0 77117-73-8 81957-76-8

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

24219-97-4	51152-88-6
81957-76-8	21535-47-7
85201-40-7	1219804-97-3
57257-81-5	71936-92-0
78684-63-6	62510-46-7