Alpha-adrenergic and 5-HT2-serotonergic effects of some beta-phenylethylamines on isolated rat thoracic aorta.
General pharmacology – January 01, 1994
Source: PubMed
Summary
2C-H demonstrated a strong ability to contract isolated rat thoracic aorta, with a potency (pD2) of 6.74, while 2C-D and homoveratrylamine showed lower potencies at 5.06 and 4.46, respectively. Notably, at a concentration of 9.9 x 10(-6) M, 2C-N acted as a competitive antagonist to serotonin. The findings suggest that the varying effects on aortic contraction among these compounds may correlate with their psychedelic properties in humans, particularly among phenylethylamines.
Abstract
1. 2C-H [2-(2,5-dimethoxyphenyl)ethylamine] (pD2 = 6.74), TMPEA [2,(2,4,5-trimethoxyphenyl)ethylamine] (pD2 = 5.83), 2C-D [2-(2,5-dimethoxy-4-methylphenyl)ethylamine] (pD2 = 5.06), homoveratrylamine [DMPEA, 2-(4,5-dimethoxyphenyl)ethylamine] (pD2 = 4.46) and homopiperonylamine [MDPEA, 2-(3,4-methylenedioxyphenyl)ethylamine] (pD2 = 4.19), elicit concentration-dependent contraction of the isolated rat thoracic aorta. 2. At 9.9 x 10(-6) M, 2C-N [2-(2,5-dimethoxy-4-nitrophenyl)ethylamine] behaves as a competitive antagonist to serotonin in this preparation. 3. Considering previous results with the structurally related 2C-B [2-(4-bromo-2,5-dimethoxyphenyl)ethylamine], weak or partial agonistic activity or antagonism of aortic contraction appears to be related to psychedelic properties reported in humans for phenylethylamines.