Alpha-adrenergic and 5-HT2-serotonergic effects of some beta-phenylethylamines on isolated rat thoracic aorta.
P Saez, Y Borges, E Gonzalez, B K Cassels
General pharmacology January 1, 1994 DOI: 10.1016/0306-3623(94)90035-3 via PubMed
Summary
AI-generated from the abstractSeveral phenylethylamine compounds cause concentration-dependent contraction of isolated rat thoracic aorta, with varying potency: 2C-H (pD2 = 6.74) is most potent, followed by TMPEA (pD2 = 5.83), 2C-D (pD2 = 5.06), homoveratrylamine (pD2 = 4.46), and homopiperonylamine (pD2 = 4.19). At a concentration of 9.9 × 10⁻⁶ M, 2C-N acts as a competitive antagonist to serotonin in this tissue. Comparing these results with earlier findings for 2C-B, weak or partial agonistic activity or antagonism of aortic contraction appears to relate to the psychedelic properties reported in humans for phenylethylamines.
Study at a glance
| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Isolated rat thoracic aorta |
| Interventions | 2C-H TMPEA 2C-D homoveratrylamine homopiperonylamine 2C-N |
| Citations | 21 |
| Key finding | Weak or partial agonistic activity or antagonism of aortic contraction by phenylethylamines appears to be related to their psychedelic properties in humans. |
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.