What question did this study set out to answer?

To characterize human 5-HT2A and 5-HT2C receptors expressed in SH-SY5Y cells and evaluate their differential activation by hallucinogenic and nonhallucinogenic ligands.

December 1, 1996Journal of Neurochemistry

Characterisation of Human 5‐Hydroxytryptamine2A and 5‐Hydroxytryptamine2C Receptors Expressed in the Human Neuroblastoma Cell Line SH‐SY5Y: Comparative Stimulation by Hallucinogenic Drugs

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Authors

RNRebecca NewtonChristus Health SPS. L. PhippsHamilton Thorne (United States)TFThomas P. FlaniganUniversity of Ulster

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Implication

In vitro study reveals selective 5-HT2A receptor activation by hallucinogens in transfected neuroblastoma cells, indicating 5-HT2A is a key mediator of hallucinogenic effects.

Key Points

To characterize human 5-HT2A and 5-HT2C receptors expressed in SH-SY5Y cells and evaluate their differential activation by hallucinogenic and nonhallucinogenic ligands.
Stably transfected the human neuroblastoma cell line SH-SY5Y with human 5-HT2A or 5-HT2C receptor cDNA.
Assessed ligand binding affinities, phosphoinositide hydrolysis, intracellular Ca2+ transients, and whole-cell membrane currents at -50 mV.
Compared activation potencies and efficacies of four hallucinogens (LSD, DOI, 5-MeO-DMT, mescaline) against three nonhallucinogens (mCPP, quipazine, ergotamine).
Serotonin stimulated phosphoinositide hydrolysis with higher potency but lower efficacy at the 5-HT2C receptor (pEC50 = 7.80 ± 0.06) compared with the 5-HT2A receptor (pEC50 = 7.30 ± 0.08).
Activation of 5-HT2A induced a transient fourfold elevation in intracellular Ca2+, while 10 µM serotonin triggered a 2 pA inward current across both receptor subtypes.
At doses yielding 20% maximal serotonin response, LSD selectively activated 5-HT2A over 5-HT2C (with weaker selectivity by DOI, mescaline, and ergotamine), whereas m-chlorophenylpiperazine selectively activated 5-HT2C.

Cite This Study

Newton et al. (1996) studied this question.

synapsesocial.com/papers/6a71b8e7e5469ee92be21be0 https://doi.org/10.1046/j.1471-4159.1996.67062521.x

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Implication

In vitro study reveals selective 5-HT2A receptor activation by hallucinogens in transfected neuroblastoma cells, indicating 5-HT2A is a key mediator of hallucinogenic effects.

Characterisation of Human 5‐Hydroxytryptamine2A and 5‐Hydroxytryptamine2C Receptors Expressed in the Human Neuroblastoma Cell Line SH‐SY5Y: Comparative Stimulation by Hallucinogenic Drugs

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Cite This Study

Characterisation of Human 5‐Hydroxytryptamine2A and 5‐Hydroxytryptamine2C Receptors Expressed in the Human Neuroblastoma Cell Line SH‐SY5Y: Comparative Stimulation by Hallucinogenic Drugs

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