Central action of Craviten (M-71)

Area of Science:

• Pharmacology
• Neuroscience

Background:

• Craviten (M-71), chemically known as 2S, 2'S) N, N'-dimethyl-N, N'-bis [1-(3', 4', 5' -trimethoxy-benzoyloxy)-butyl-2]-ethylenediamine dihydrochloride, is recognized for its potent antiarrhythmic properties.

Purpose of the Study:

• To investigate the central nervous system (CNS) effects of Craviten.
• To evaluate the impact of Craviten on various physiological parameters including motor activity, analgesia, anticonvulsant activity, body temperature, arterial blood pressure, and respiration.

Main Methods:

• Assessment of spontaneous motor activity and amphetamine-induced hyperactivity in rats and mice.
• Evaluation of rota-rod performance for motor coordination.
• Testing for analgesic and anticonvulsant effects.
• Measurement of hexobarbital sleeping time.
• Monitoring of body temperature, arterial blood pressure, and respiration in rats and mice.

Main Results:

• Craviten exhibited no discernible effects on spontaneous motor activity, amphetamine-stimulated hyperactivity, rota-rod performance, analgesic, or anticonvulsant activities.
• No alterations in hexobarbital sleeping time or body temperature were observed in rodents.
• A dose-dependent decrease in arterial blood pressure and slight respiratory stimulation were noted in rats.
• LD50 values were determined: rats (142 mg/kg ip, 15 x 8 mg/kg iv), mice (550 mg/kg ip), and rabbits (5 x 1 mg/kg iv).

Conclusions:

• Craviten, despite its antiarrhythmic action, does not appear to possess significant central nervous system activity in rodents.
• The observed hypotensive and respiratory effects warrant further investigation.
• The determined LD50 values provide crucial data for safety and dosage considerations.