Related Experiment Video
Updated: Jun 6, 2025
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Creating Dynamic Images of Short-lived Dopamine Fluctuations with lp-ntPET: Dopamine Movies of Cigarette Smoking
Published on: August 6, 2013
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Neurochemical characterization of 5-HT2AR partial agonists with simultaneous PET-MRI
Frederick A Bagdasarian1, Kristian Larsen2,3, Hong Ping Deng1
1Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, USA.
Summary
Serotonin 2A receptor (5-HT2AR) agonists like psilocybin and lisuride showed varied brain blood flow responses. Different drug profiles impact therapeutic potential for psychiatric conditions.
Area of Science:
- Neuroscience
- Pharmacology
- Psychiatry
Background:
- Serotonin 2A receptor (5-HT2AR) agonists are investigated for psychiatric treatments.
- Understanding their diverse pharmacological profiles is crucial for drug development.
Purpose of the Study:
- To investigate the neuromodulatory effects of psilocybin, lisuride, and 25CN-NBOH on 5-HT2AR.
- To compare their receptor occupancy and cerebral blood volume (CBV) changes using simultaneous PET and phMRI.
Main Methods:
- Simultaneous positron emission tomography (PET) and pharmacological magnetic resonance imaging (phMRI) in nonhuman primates (N=3).
- Assessment of 5-HT2AR occupancy with [11C]MDL-100907 PET.
- Measurement of cerebral blood volume (CBV) changes with phMRI.
Main Results:
- Mixed agonists psilocybin and lisuride induced biphasic CBV responses; selective 25CN-NBOH caused monophasic increases.
- Psilocybin and lisuride showed similar cortical 5-HT2AR occupancy at tested doses.
- 25CN-NBOH had lower occupancy but greater CBV changes than psilocybin and lisuride.
Conclusions:
- Hemodynamic responses vary based on agonist affinity profiles, influencing therapeutic applications.
- Findings offer insights into the pharmacological impacts of serotonergic agonists for psychiatric conditions.
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