Dimetotiazine

Modify Date: 2024-01-13 22:07:43

Dimetotiazine Structure
Dimetotiazine structure
Common Name Dimetotiazine
CAS Number 7456-24-8 Molecular Weight 391.55100
Density 1.235g/cm3 Boiling Point 533.7ºC at 760 mmHg
Molecular Formula C19H25N3O2S2 Melting Point N/A
MSDS N/A Flash Point 276.6ºC

 Use of Dimetotiazine


Dimethothiazine (Dimetotiazine; Fonazine) is an orally active tricyclic anti-histamine, anti-5-HT agent with a high activity against decerebrate rigidity, a little sedative activity and little soporific action. Dimethothiazine can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine can be used to research hemicrania and spasticity[1][2][3].

 Names

Name 10-[2-(dimethylamino)propyl]-N,N-dimethylphenothiazine-2-sulfonamide
Synonym More Synonyms

 Dimetotiazine Biological Activity

Description Dimethothiazine (Dimetotiazine; Fonazine) is an orally active tricyclic anti-histamine, anti-5-HT agent with a high activity against decerebrate rigidity, a little sedative activity and little soporific action. Dimethothiazine can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine can be used to research hemicrania and spasticity[1][2][3].
Related Catalog
Target

Histamine, 5-HT[1]

In Vivo Dimethothiazine (0.5-16 mg/kg; i.v.; single dosage) reduces decerebrate rigidity in cats[2]. Animal Model: Cats (decerebrate model; the carotid arteries were clamped and the mid-brain sectioned approximately between the colliculae)[2] Dosage: 0.5, 1, 2, 4, 8 and 16 mg/kg Administration: i.v.; single dosage Result: Reduced the discharge frequency of primary and secondary endings at 1-4 mg/kg. Reduced the sensitivity of the muscle spindle to stretch in preparations with intact ventral roots. Reduced the activity of the dynamic fusimotor fibres.
References

[1]. Nattero G, et al. Use of dimethothiazine in the prevention of hemicrania. Minerva Med. 1977 Mar 17;68(13):839-45.

[2]. Maxwell DR, Rhodes KF. The effects of dimethothiazine on muscle spindle activity in the decerebrate cat. Br J Pharmacol. 1970 Jul;39(3):520-32.

[3]. Griffiths MI, et al. The use of dimethothiazine in the treatment of childhood cerebral palsy. Dev Med Child Neurol. 1973 Feb;15(1):25-32.

 Chemical & Physical Properties

Density 1.235g/cm3
Boiling Point 533.7ºC at 760 mmHg
Molecular Formula C19H25N3O2S2
Molecular Weight 391.55100
Flash Point 276.6ºC
Exact Mass 391.13900
PSA 77.54000
LogP 4.63550
Index of Refraction 1.612

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SP5250000
CHEMICAL NAME :
Phenothiazine-2-sulfonamide, 10-(2-(dimethylamino)propyl)-N,N-dimethyl-
CAS REGISTRY NUMBER :
7456-24-8
LAST UPDATED :
199612
DATA ITEMS CITED :
5
MOLECULAR FORMULA :
C19-H25-N3-O2-S2
MOLECULAR WEIGHT :
391.59
WISWESSER LINE NOTATION :
T C666 BN ISJ B1Y1&N1&1 ESWN1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
740 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 159,70,1966
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
190 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 159,70,1966
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
475 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 159,70,1966
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
100 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 159,70,1966 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
600 mg/kg
SEX/DURATION :
female 9-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 4,381,1970

 Synonyms

dimethothiazine
FONAZINE
Dimetiotazine
Dimethodin
10-(2-dimethylamino-propyl)-10H-phenothiazine-2-sulfonic acid dimethylamide
Dimetotiazinum [INN-Latin]
N,N-Dimethyl-10-(2-dimethylaminopropyl)-phenothiazin-2-sulfonamide
Dimetotiazine
Dimetotiazine [INN:BAN]
Bayer 1483
Dimetotiazina [INN-Spanish]
Dimetiotazin
Dimethothiazin