OBSERVATIONS ON SEVERAL CYCLOHEXYL- AND PHENYL-ALKYLAMINES

¹ Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pa., and Research Division, Smith, Kline and French Laboratories, Philadelphia, Pa.
² Research Division, Smith, Kline and French Laboratories, Philadelphia, Pennsylvania

In the present studies, the pharmacological actions of 1-cyclohexyl-2-amino-propane (No. 10) and 1-cyclohexyl-2-methylaminopropane (No. 25, the N-methyl modification of No. 10) have been compared with their corresponding phenyl analogues (No. 1 and No. 4).

See table in the PDF file

1. Observations in rats, rabbits and guinea pigs disclosed the fact that the cyclohexyl derivatives were decidedly less active central nervous system stimulants than their corresponding phenyl modifications.

2. In dogs anesthetized with pentobarbital sodium and prepared to record carotid blood pressure by means of a mercury manometer, No. 10 and No. 25 exhibited one-half the intravenous pressor potency of No. 1 or No. 4.

3. Intravenously 0.2 to 0.3 mgm. of No. 25 caused a slight increase in the amplitude of cardiac contraction as determined by a Cushny Myocardiograph and a slight increase in heart rate.

4. Photoelectric or impedance volume pulses disclosed that No. 25 exhibited peripheral vasoconstrictor activity.

5. Direct application of the free base of No. 25 to the nasal mucosa of dogs disclosed the fact that it exhibited essentially the same order of vasoconstrictor activity as did the free base of No. 1 in the present experiments.

6. No signs of irritation were apparent on histological examination of the sections of the tracheo-bronchial tree of rats which were allowed to inhale fixed doses of the free base of No. 25 daily for thirty days.

7. Rats, rabbits and guinea pigs received daily injections of large doses of No. 25 for thirty days. No evidence of histological damage was apparent after examination of the tissues removed from these animals.

8. The data obtained in the present experiments suggested that the free base of No. 25 be used clinically as a volatile vasoconstrictor agent.