(±)-1-(2,5-Dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), a novel putative anxiolytic agent lacking affinity for benzodiazepine sites and serotonin-1A receptors Export

@article{citeulike:3388196, abstract = {Serotonergic behavioral responses, effects on motor activity and core temperature, and binding properties of the novel putative anxiolytic amphetamine derivative (±)1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), were examined in rodents in order to elucidate the mechanism underlying its anxiolytic-like effect. After peripheral administration in rats, ALEPH-2 induced some symptoms of the serotonergic syndrome, e.g. forepaw treading and flat body posture. Additionally, a decrease in motor activity was observed. No significant effects on the number of head shakes were observed after injection, although high inter-subject variability was noted. Higher doses of ALEPH-2, in the range exhibiting anxiolytic properties (4mg/kg), elicited significant hypothermia in mice. The affinity of the drug for 5-HT2A/2C receptors ([3H]ketanserin sites) was in the nanomolar range (Ki = 173 nM), whereas for 5-HT1A, benzodiazepine sites, and GABAA receptors, the affinity was micromolar or lower. Based on these results the mechanism of action and the anxiolytic-like properties of ALEPH-2 are discussed.}, author = {Reyes-Parada, Miguel and Scorza, Cecilia and Romero, Ver\'{o}nica and Silveira, Rodolfo and Medina, Jorge H. and Andrus, Danice and Nichols, David E. and Cassels, Bruce K.}, citeulike-article-id = {3388196}, citeulike-linkout-0 = {http://dx.doi.org/10.1007/BF00170831}, day = {1}, doi = {10.1007/BF00170831}, journal = {Naunyn-Schmiedeberg's Archives of Pharmacology}, keywords = {5ht-2c, aleph-2, anxiolytic}, month = {November}, number = {5}, pages = {579--585}, posted-at = {2008-10-08 19:43:07}, priority = {5}, title = {(±)-1-(2,5-Dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), a novel putative anxiolytic agent lacking affinity for benzodiazepine sites and serotonin-1A receptors}, url = {http://dx.doi.org/10.1007/BF00170831}, volume = {354}, year = {1996} }

TY - JOUR ID - citeulike:3388196 L3 - citeulike-article-id:3388196 N2 - Serotonergic behavioral responses, effects on motor activity and core temperature, and binding properties of the novel putative anxiolytic amphetamine derivative (±)1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), were examined in rodents in order to elucidate the mechanism underlying its anxiolytic-like effect. After peripheral administration in rats, ALEPH-2 induced some symptoms of the serotonergic syndrome, e.g. forepaw treading and flat body posture. Additionally, a decrease in motor activity was observed. No significant effects on the number of head shakes were observed after injection, although high inter-subject variability was noted. Higher doses of ALEPH-2, in the range exhibiting anxiolytic properties (4mg/kg), elicited significant hypothermia in mice. The affinity of the drug for 5-HT2A/2C receptors ([3H]ketanserin sites) was in the nanomolar range (Ki = 173 nM), whereas for 5-HT1A, benzodiazepine sites, and GABAA receptors, the affinity was micromolar or lower. Based on these results the mechanism of action and the anxiolytic-like properties of ALEPH-2 are discussed. IS - 5 JF - Naunyn-Schmiedeberg's Archives of Pharmacology EP - 585 TI - (±)-1-(2,5-Dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), a novel putative anxiolytic agent lacking affinity for benzodiazepine sites and serotonin-1A receptors VL - 354 SP - 579 KW - 5ht-2c KW - aleph-2 KW - anxiolytic AU - Reyes-Parada, Miguel AU - Scorza, Cecilia AU - Romero, Verónica AU - Silveira, Rodolfo AU - Medina, Jorge AU - Andrus, Danice AU - Nichols, David AU - Cassels, Bruce PY - 1996/11/01/ UR - http://dx.doi.org/10.1007/BF00170831 ER -