Characterisation of human 5-hydroxytryptamine2A and 5-hydroxytryptamine2C receptors expressed in the human neuroblastoma cell line SH-SY5Y: comparative stimulation by hallucinogenic drugs.
Journal of neurochemistry December 1, 1996 R A Newton, S L Phipps, T P Flanigan et al. 46 citations
Cell lines engineered to express human 5-HT2A or 5-HT2C receptors showed ligand binding similar to natural receptors in brain tissue. Serotonin triggered stronger but less effective phosphoinositide signaling at 5-HT2C than at 5-HT2A receptors, and 5-HT2A activation briefly raised intracellular calcium fourfold. Both receptors produced a tiny inward current when stimulated. Among hallucinogens (LSD, DOI, DMT, mescaline) and nonhallucinogens, no differences in phosphoinositide signaling potency or efficacy emerged. LSD and DOI preferentially activated 5-HT2A, while m-CPP activated 5-HT2C. The findings suggest hallucinosis is not primarily mediated by 5-HT2C activity; 5-HT2A activation may be important but not the sole mechanism.