Alpha-adrenergic and 5-HT2-serotonergic effects of some beta-phenylethylamines on isolated rat thoracic aorta.
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.
Departamento de Química, Facultad de Ciencias, Universidad de Chile, Santiago.
P
P
Saez
Y
Y
Borges
E
E
Gonzalez
B K
BK
Cassels
D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects* / Q000648:ultrastructure*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D010627:Phenethylamines / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects*; D011985:Receptors, Serotonin / Q000187:drug effects*; D014662:Vasoconstrictor Agents / Q000494:pharmacology
D010627:Phenethylamines; D018340:Receptors, Adrenergic, alpha-1; D011985:Receptors, Serotonin; D014662:Vasoconstrictor Agents