Pimethixene maleate

Names

[ Name ]:
Pimethixene maleate

[Synonym ]:
1-Methyl-4-(thioxanthen-9-ylidene)piperidine
PIMETHIXEN MALEATE SALT
1-methyl-4-(9H-thioxanthen-9-ylidene)piperidinium hydrogen maleate
9-(1-methyl-4-piperidylene)thioxanthenemaleate
9-(1-methyl-4-piperidylene)-thioxanthenmaleate
PIMETHIXENE MALEATE SALT
bp-400
9-(n-methyl-piperidyliden-4)thioxanemaleate
Pimethixene maleic salt
PIMETHIXENE MALEATE

Biological Activity

[Description]:

Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Signaling Pathways >> GPCR/G Protein >> mAChR

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

pKi: 7.63 (5-HT1A receptor), 10.22 (5-HT2A receptor), 10.44 (5-HT2B receptor), 8.42 (5-HT2C receptor), 10.14 (histamine H1 receptor), 8.19 (D2 receptor), 7.54 (DD4.4 receptor), 8.61 (M1 receptor), 9.38 (M2 receptor)[1]

[References]

[1]. Schmitz B, et al. BF-1--a novel selective 5-HT2B receptor antagonist blocking neurogenic dural plasma protein extravasation in guinea pigs. Eur J Pharmacol. 2015 Mar 15;751:73-80.

Chemical & Physical Properties

[ Density]:
1.192g/cm3

[ Boiling Point ]:
439.7ºC at 760mmHg

[ Molecular Formula ]:
C₂₃H₂₃NO₄S

[ Molecular Weight ]:
409.50

[ Flash Point ]:
219.7ºC

[ Exact Mass ]:
409.13500

[ PSA ]:
103.14000

[ LogP ]:
4.32840

[ Vapour Pressure ]:
5.08E-17mmHg at 25°C

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XO0782000

CHEMICAL NAME :: Thioxanthene, 9-(1-methyl-4-piperidylene)-, maleate

CAS REGISTRY NUMBER :: 13187-06-9

LAST UPDATED :: 199709

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C19-H19-N-S.C4-H4-O4

MOLECULAR WEIGHT :: 409.53

WISWESSER LINE NOTATION :: T C666 BS IYJ IU- DT6N DYTJ A1 &QV1U1VQ -C

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 :: 1186 mg/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18 mg/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 433 mg/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31400 ug/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 25 mg/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9100 mg/kg/13W-I

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Related to Chronic Data - death

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xn: Harmful;

[ Risk Phrases ]:
22-36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ RTECS ]:
XO0782000

[ HS Code ]:
2934999090

Customs

[ HS Code ]: 2934999090

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

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.