Erowid References Database
Edwards E, Ashby CR, Wang RY.
“±-1-2,5-Dimethoxy-4-iodophenyl-2-aminopropaneDOI and alpha-methyl-5-HT: 5-HT2 receptor agonistic action on phosphatidylinositol metabolism in the rat fronto-cingulate and entorhinal cortex”.
Neuropharmacology. 1992 Jul 06;31(7):615-21.
In the present study, the effects of 5-HT and two 5-HT1c/5-HT2 receptor agonists, ±-1-2,5-dimethoxy-4-iodophenyl-2-aminopropane DOI and alpha-methyl-serotonin alpha-Me-5-HT on phosphoinositide hydrolysis were compared, to determine whether DOI and alpha-Me-5-HT were full agonists. Consistent with the results obtained from previous studies, both ±-DOI and alpha-Me-5-HT stimulated turnover of phosphoinositide in a concentration-dependent manner. However, the response obtained with these 5-HT1c/5-HT2 receptor agonists was only 30-40 of that of 5-HT. The stimulation of hydrolysis of phosphoinositide, produced by both 5-HT2 receptor agonists, was potently antagonized by ritanserin a 5-HT1c/5-HT2 receptor antagonist and alpha-phenyl-1-2-phenylethyl-4-piperine methanol [+-MDL 11,939, a 5-HT2 receptor antagonist] but not by granisetron BRL a 5-HT3 receptor antagonist, suggesting that the action of DOI and alpha-Me-5-HT was primarily mediated by 5-HT2 receptors. When the effect of increasing the concentration of 5-HT on turnover of phosphoinositide was measured in the presence of a 1 microM concentration of the 5-HT3 receptor antagonist granisetron, the response obtained was similar to the response produced by the 5-HT2 receptor agonists, DOI and alpha-Me-5-HT. These results confirm the previous finding that 5-HT stimulates hydrolysis of phosphoinositide by interacting with 5-HT1c/5-HT2 and 5-HT3 receptors. Moreover, they suggest that DOI and alpha-Me-5-HT are full agonists at the 5-HT2 receptor, coupled to hydrolysis of phosphoinositide in the cortex of the rat.
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