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Product Name: AZAPHEN
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24853-80-3

24853-80-3 structure

Name: Azaphen
Chemical Name: 5-methyl-3-(4-methylpiperazin-1-yl)pyridazino[3,4-b][1,4]benzoxazine,dihydrochloride
CAS Number: 24853-80-3
Molecular Formula: C₁₆H₂₁Cl₂N₅O
Molecular Weight: 370.27700
Catalog: Signaling Pathways Neuronal Signaling Serotonin Transporter
Create Date: 2018-05-17 08:00:00
Modify Date: 2024-01-08 17:28:48
Pipofezine(Azafen or Azaphen) is a potent inhibitor of the reuptake of serotonin. IC50 Value: Target: SSRIsPipofezine is a tricyclic antidepressant (TCA) approved in Russia for the treatment of depression. In addition to its antidepressant action, pipofezine has sedative effects as well, indicating antihistamine activity.

Name	5-methyl-3-(4-methylpiperazin-1-yl)pyridazino[3,4-b][1,4]benzoxazine,dihydrochloride
Synonyms	Azaphenonxazine 2HCl 5-methyl-3-(4-methyl-piperazin-1-yl)-5H-benzo[b]pyridazino[4,3-e][1,4]oxazine,dihydrochloride 5H-Pyridazino(3,4-b)(1,4)benzoxazine,5-methyl-3-(4-methyl-1-piperazinyl)-,dihydrochloride 5-Methyl-3-(4-methyl-1-piperazinyl)-5H-pyridazino(3,4-b)(1,4)benzoxazine dihydrochloride Azaphen hydrochloride Azafen 2-(4-Methyl-1-piperazinyl)-10-methyl-3,4-diazaphenoxazindihydrochlorid [German] pipofezine,dihydrochloride Pipofezin hydrochloride 5-methyl-3-(4-methylpiperazin-1-yl)-5h-pyridazino[3,4-b][1,4]benzoxazine dihydrochloride Azaphen

Description	Pipofezine(Azafen or Azaphen) is a potent inhibitor of the reuptake of serotonin. IC50 Value: Target: SSRIsPipofezine is a tricyclic antidepressant (TCA) approved in Russia for the treatment of depression. In addition to its antidepressant action, pipofezine has sedative effects as well, indicating antihistamine activity.
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter Research Areas >> Neurological Disease Natural Products >> Alkaloid
References	[1]. Domestic antidepressants. 1. Azaphen By Andreeva, N. I.; Asnina, V. V.; Liberman, S. S. From Pharmaceutical Chemistry Journal (Translation of Khimiko-Farmatsevticheskii Zhurnal) (2000), 34(5), 237-241. [2]. Shinaev NN, Akzhigitov RG. Azaphen: a return to clinical practice.Zh Nevrol Psikhiatr Im S S Korsakova. 2005;105(10):55-6. [3]. Ignatowicz L, Ignatowicz R, Wdowiak MW, Jaremko A. Azaphen in the treatment of enuresis in children.Psychiatr Pol. 1977 Jan-Feb;11(1):29-33. [4]. Liberman SS, Sharova SA. A comparison of the effect of the tricyclic antidepressants azaphen and imizin on the gastrointestinal tracts of experimental animals.Farmakol Toksikol. 1975 Jan-Feb;38(1):29-32. [5]. Misurec J, Náhunek K, Kamenická V, Chmelar M. Proceedings: Influence of azaphen, a new antidepressive drug, on the human EEG. Act Nerv Super (Praha). 1974;16(4):245-6.

Boiling Point	536ºC at 760 mmHg
Molecular Formula	C₁₆H₂₁Cl₂N₅O
Molecular Weight	370.27700
Flash Point	278ºC
Exact Mass	369.11200
PSA	44.73000
LogP	3.77390
Vapour Pressure	1.46E-11mmHg at 25°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UR6080000

CHEMICAL NAME :: 5H-Pyridazino(3,4-b)(1,4)benzoxazine, 5-methyl-3-(4-methyl-1-piperazinyl)-, dihydrochloride

CAS REGISTRY NUMBER :: 24853-80-3

LAST UPDATED :: 199706

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C16-H19-N5-O.2Cl-H

MOLECULAR WEIGHT :: 370.32

WISWESSER LINE NOTATION :: T C666 BO DNN INJ I1 F- AT6N DNTJ D1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1 gm/kg

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

REFERENCE :: ZPPLBF Zentralblatt fuer Pharmazie, Pharmakotherapie und Laboratoriums-diagnostik. (VEB Verlag Volk und Gesundheit, Neue Gruenstr. 18, 102 Berlin, Ger. Dem. Rep.) V.109- 1970- Volume(issue)/page/year: 114,787,1975

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 490 mg/kg

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

REFERENCE :: ZPPLBF Zentralblatt fuer Pharmazie, Pharmakotherapie und Laboratoriums-diagnostik. (VEB Verlag Volk und Gesundheit, Neue Gruenstr. 18, 102 Berlin, Ger. Dem. Rep.) V.109- 1970- Volume(issue)/page/year: 114,787,1975

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 48 mg/kg

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

REFERENCE :: ZPPLBF Zentralblatt fuer Pharmazie, Pharmakotherapie und Laboratoriums-diagnostik. (VEB Verlag Volk und Gesundheit, Neue Gruenstr. 18, 102 Berlin, Ger. Dem. Rep.) V.109- 1970- Volume(issue)/page/year: 114,787,1975

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 700 mg/kg

TOXIC EFFECTS :: Behavioral - wakefulness

REFERENCE :: PCJOAU Pharmaceutical Chemistry Journal (English Translation). Translation of KHFZAN. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No.1- 1967- Volume(issue)/page/year: 4,118,1970

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 330 mg/kg

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: ZPPLBF Zentralblatt fuer Pharmazie, Pharmakotherapie und Laboratoriums-diagnostik. (VEB Verlag Volk und Gesundheit, Neue Gruenstr. 18, 102 Berlin, Ger. Dem. Rep.) V.109- 1970- Volume(issue)/page/year: 114,787,1975

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 63 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: RPTOAN Russian Pharmacology and Toxicology (English Translation). Translation of FATOAO. (Euromed Pub., 33, Woodlands Rd., Surbiton, Surrey, UK) V.30- 1967- Volume(issue)/page/year: 37,2,1974

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 200 mg/kg

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

REFERENCE :: ZPPLBF Zentralblatt fuer Pharmazie, Pharmakotherapie und Laboratoriums-diagnostik. (VEB Verlag Volk und Gesundheit, Neue Gruenstr. 18, 102 Berlin, Ger. Dem. Rep.) V.109- 1970- Volume(issue)/page/year: 114,787,1975

HS Code	2934999090

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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