Possible Interaction: Cocaine and Ketanserin

“This effect was prevented when cocaine was co-administered with the selective 5-HT2A receptor antagonist ketanserin and was mimicked by repeated 5-HT2A receptor agonist (−)4-iodo-2,5-dimethoxyphenylisopropylamine administration.”

“In summary, Acute studies showed that cocaine produced its psychostimulant responses on monoamines and behavior and ketanserin antagonized these responses, likely via a 5-HT(2A/2C) receptor mediation.”

“ Ketanserin (3.0 mg/kg) also produced a significant shift to the right of the cocaine dose-response curve and antagonized increases in rates of responding produced by lower doses of cocaine.”

“The ability of (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), a 5-HT(2A) receptor agonist, and ketanserin , a 5-HT(2A) receptor antagonist, to either substitute for or block the discriminative-stimulus effects of cocaine , or to shift the cocaine dose-response curve, was evaluated.”

“M100907 (0.05-1.6 mg/kg) and ketanserin (0.05-4 mg/kg) evoked a dose-related attenuation of the stimulus effects of cocaine (5 mg/kg, p < 0.05).”

“In animals treated repeatedly with the psychostimulant, the behavioral response to a challenge dose of cocaine was dose-dependently decreased when the drug was combined with ketanserin , but not with prazosin.”

“In drug interaction studies, the 5HT uptake inhibitors and quipazine produced an insurmountable attenuation of the behavioral-stimulant effects of cocaine, whereas the 5HT antagonists ketanserin , mianserin and ritanserin) with high affinity for 5HT2 binding sites enhanced the behavioral-stimulant effects of low or intermediate doses of cocaine.”

“Pretreatment with the D1 antagonist SCH23390, the D2 antagonist sulpiride, the D1/D2 antagonist fluphenazine, or the 5-HT2 antagonist ketanserin significantly decreased the ACTH elevations after cocaine.”