Pizotifen malate

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

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

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

Research Areas >> Neurological Disease

Natural Products >> Alkaloid

5-HT2A Receptor

5-HT1C Receptor

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].

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].

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].

[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.

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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