A multimodal neuroimaging agent for human 5-HT1A/5-HT7 receptors

The 5-HT1A and 5-HT7 receptors are highly co-expressed as monomers and oligomers in specific brain regions and responsible for modulating serotonergic signaling. Under depressed conditions, the signaling of 5-HT1A receptors gets modulated by 5-HT7 receptors in the central nervous system. This complex signaling mechanism includes structural reorganizations such as dimerization, altering the synaptic gradient of these receptors. Hence, imaging of 5-HT1A/5-HT7 receptors either inmonomeric or dimeric states under physiological and pathological environment can be employed to track the quantitative/functional facet of neurological disorders. At present, we report design and development of a multimodal ¹¹C-PET/^99mTc-single photon emission computed tomography-based radioligands for targeted in vivo imaging of human 5-HT1A/5- HT7 neurotransmitters. A new multimodal positron emission tomography/single photon emission computed tomography-based brain imaging agent was screened and synthesized to selectively map the h5-HT1A/5-HT7 receptors. Substantial brain permeation and favored radioactivity accumulation in specific receptor-rich brain regions were observed in the preclinical evaluations, suggesting promising venture for delineating neurological disorders