Towards selective CNS PET Imaging of the 5-HT7 Receptor System: Past, Present and Future.

Towards selective CNS PET Imaging of the 5-HT7 Receptor System: Past, Present and Future. Neuropharmacology. 2019 Oct 24;:107830 Authors: L'Estrade ET, Erlandsson M, Edgar FG, Ohlsson T, Knudsen GM, Herth MM Abstract Since its discovery in 1993, the serotonin receptor subtype 7 (5-HT7) has attracted significant attention as a potential drug target; due to its elucidated roles in conditions such as insomnia, schizophrenia, and more. Therefore, it is unsurprising that there has been relatively early efforts undertaken to develop a positron emission tomography (PET) imaging agent for said receptor system. PET can be clinically used to probe receptor systems in vivo, permitting information such as a drug's occupancy against this system to be investigated. This review focuses on the efforts towards the development of a 5-HT7R selective PET CNS tracer over the last 20 years, critically reflecting on applied strategies and commonly employed chemical frameworks and suggests future considerations that are needed to successfully develop a PET tracer for this clinically relevant target. PMID: 31669129 [PubMed - as supplied by publisher]
Source: Neuropharmacology - Category: Drugs & Pharmacology Authors: Tags: Neuropharmacology Source Type: research