Pizotifen malate

Modify Date: 2024-01-02 11:24:53

Pizotifen malate Structure
Pizotifen malate structure
 Common Name Pizotifen malate
CAS Number 5189-11-7 Molecular Weight 429.53
Density N/A Boiling Point 436.7ºC at 760 mmHg
Molecular Formula C23H27NO5S Melting Point 185-186° (dec)
MSDS N/A Flash Point 217.9ºC

 Use of Pizotifen malate


Pizotifen malate is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.

 Names

Name pizotifen malate
Synonym More Synonyms

 Pizotifen malate Biological Activity

Description Pizotifen malate is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
Related Catalog
Target

5-HT2A Receptor

5-HT1C Receptor

In Vitro Pizotifen is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site[1]. Pizotifen is an antidepresent 5-HT2A receptor antagonist and has the capacity to inhibit serotonin-enhanced ADP-induced platelet aggregation[2].
In Vivo The weights of the fetuses are significantly reduced by all administered doses of Pipethiadene and Pizotifen malate; the weights of the placentas are significantly reduced after 0.6 and 1.2 mg/kg Pipethiadene and only after the middle dose of Pizotifen malate. The means of the implantations, live, dead fetuses, resorptions and the occurrence of external, skeletal and visceral anomalies do not differ from the control group. The number of chromosome aberrations in the bone marrow cells of treated mice does not differ significantly from the negative control group. The micronucleus test reveals no elevation in the frequency of micronuclei as compared to the control group. After the two higher doses of both Pipethiadene and Pizotifen maleate, the mitotic indices are lower than in the control group[3].
Animal Admin Mice[3] Pizotifen malate is administered orally to three groups of Swiss mice in doses of 0.24, 0.6 and 1.2 mg/kg from day 4 to day 16 of gestation. The control group is treated with distilled water. On day 19 of gestation, the mice are sacrificed and cytogenetical examination and uterine content (number of live, abnormal and dead fetuses as well as the number of implantations, resorptions) are determined. The live fetuses were inspected for external, visceral and skeletal malformations[3].
References

[1]. Mylecharane EJ, et al. 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52.

[2]. Lin OA, et al. The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026.

[3]. Ujházy E, et al. Teratological and cytogenetical evaluation of two antihistamines (pipethiadene and pizotifen maleate) in mice. Agents Actions. 1988 Apr;23(3-4):376-8.

 Chemical & Physical Properties

Boiling Point 436.7ºC at 760 mmHg
Melting Point 185-186° (dec)
Molecular Formula C23H27NO5S
Molecular Weight 429.53
Flash Point 217.9ºC
PSA 106.08000
LogP 4.02390
Storage condition 2–8 °C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TM7165500
CAS REGISTRY NUMBER :
5189-11-7
LAST UPDATED :
198910
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C19-H21-N-S.C4-H6-O5
MOLECULAR WEIGHT :
429.57
WISWESSER LINE NOTATION :
T C576 BY FS&T&J BU- DT6N DYTJ A1 &QV1U1VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
600 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - visual field changes Cardiac - pulse rate increase, without fall in BP Nutritional and Gross Metabolic - body temperature increase
REFERENCE :
PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 63,59,1987
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
17 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 19,19,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
43 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 19,19,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
19 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 19,19,1969

 Safety Information

Hazard Codes Xi
Risk Phrases 36/37/38
Safety Phrases 26-37/39
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%

 Synonyms

4-(9,10-Dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene)-1-methylpiperidine (2Z)-2-butenedioate (1:1)
4-(9,10-Dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene)-1-methylpiperidinium hydrogen (2Z)-but-2-enedioate (1:1:1)
Sanomtgran
Sandomigran malate
4-(4,5-dihydrobenzo[1,2]cyclohepta[3,4-b]thiophen-10-ylidene)-1-methylpiperidine,2-hydroxybutanedioic acid
Litec malate
Piperidine, 4-(9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thien-4-ylidene)-1-methyl-, (2Z)-2-butenedioate (1:1)
Pizotyline malate
Pizotifen hydrogen malate
Pizotifen malate
Mosegor
Sandomygran malate
Sandomigran
piperidinium, 4-(9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thien-4-ylidene)-1-methyl- (2Z)-2-butenedioate, hydrogen salt (1:1:1)
Sandomigran,pizotyline
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