50335-55-2

50335-55-2 structure

Name: Mezilamine
Chemical Name: Mezilamine
CAS Number: 50335-55-2
Molecular Formula: C₁₁H₁₈ClN₅S
Molecular Weight: 287.81200
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2017-11-17 23:03:43
Modify Date: 2024-01-02 11:20:09
Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of 3H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist[1].

Name	Mezilamine
Synonyms	4-Chloro-2-methylamino-5-methylthio-6-(4-methyl-1-piperazinyl)pyrimidine [4-chloro-6-(4-methyl-piperazin-1-yl)-5-methylsulfanyl-pyrimidin-2-yl]-methyl-amine N-Methyl-4-chloro-5-(methylthio)-6-(4-methylpiperazino)pyrimidine-2-amine 4-Chloro-N-methyl-6-(4-methylpiperazin-1-yl)-5-(methylthio)pyrimidin-2-amine 2-Methylamino-4-(4-methylpiperazino)-5-methylmercapto-6-chlorpyrimidin

Description	Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of 3H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist[1].
Related Catalog	Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Neurological Disease
In Vitro	Mezilamine (1, 5, 10 μM) 导致 3H 刺激的溢出浓度依赖性增加，而不影响皮质切片的自发流出[1]。
References	[1]. G Le Fur, et al. Mezilamine, a new dopamine antagonist, blocks presynaptic but stimulates postsynaptic alpha-adrenoceptors. Eur J Pharmacol. 1979 Oct 15;58(4):359-67.

Density	1.32g/cm3
Boiling Point	440.2ºC at 760 mmHg
Molecular Formula	C₁₁H₁₈ClN₅S
Molecular Weight	287.81200
Flash Point	220ºC
Exact Mass	287.09700
PSA	69.59000
LogP	1.72130
Index of Refraction	1.627

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV8126000

CHEMICAL NAME :: Pyrimidine, 4-chloro-2-(methylamino)-5-(methylthio)-6-(4-methyl-1 -piperazinyl)-

CAS REGISTRY NUMBER :: 50335-55-2

BEILSTEIN REFERENCE NO. :: 0666978

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C11-H18-Cl-N5-S

MOLECULAR WEIGHT :: 287.85

WISWESSER LINE NOTATION :: T6N DNTJ A1 D- DT6N CNJ BM1 ES1 FG

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 :: 800 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,742,1977

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 21 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,742,1977

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 330 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,742,1977

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 2,742,1977

HS Code	2933990090

109-01-3

40765-72-8

50335-55-2

Literature: Gueremy, Claude; Audiau, Francois; Uzan, Andre; Fur, Gerard Le; Leger, Jean-Michel; Carpy, Alain Journal of Medicinal Chemistry, 1982 , vol. 25, # 12 p. 1459 - 1465

Precursor 2
109-01-3 40765-72-8
DownStream 0

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%

50335-55-2	50295-40-4
1158522-08-7	940364-43-2
1342994-82-4	134104-43-1
116137-76-9	1269504-32-6
131615-57-1	6906-52-1
1341117-68-7	930439-75-1