General pharmacology
January 1, 1994
P Saez, Y Borges, E Gonzalez et al.
21 citations
Several 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.
Naunyn-Schmiedeberg's archives of pharmacology
November 1, 1996
M Reyes-Parada, C Scorza, V Romero et al.
6 citations
The novel amphetamine derivative ALEPH-2, a putative anxiolytic, produced serotonergic syndrome symptoms like forepaw treading and flat body posture in rats, along with decreased motor activity. No significant effect on head shakes was observed, though variability was high. In mice, higher doses (4 mg/kg) caused significant hypothermia. The drug showed nanomolar affinity for 5-HT2A/2C receptors (Ki = 173 nM) but only micromolar or lower affinity for 5-HT1A, benzodiazepine, and GABAA receptors. These findings suggest ALEPH-2's anxiolytic-like effects involve serotonergic mechanisms, particularly 5-HT2A/2C receptor interactions.
Life sciences
November 17, 2000
C Acuña-castillo, C Scorza, M Reyes-Parada et al.
3 citations
ALEPH-2, a phenylisopropylamine derivative with claimed anxiolytic and hallucinogenic effects, acts as a partial agonist on the 5-HT2A receptor with potency similar to serotonin, but as a full agonist on the 5-HT2C receptor, where it is about 15-fold less potent than serotonin. The antagonist ritanserin blocks responses to both serotonin and ALEPH-2 equally, though the 5-HT2A receptor is more sensitive to ritanserin than the 5-HT2C receptor.