Synthesis and evaluation of two new candidate high-affinity full agonist PET radioligands for imaging 5-HT_1B receptors.

ABSTRACT:

Introduction

The serotonin 1B receptor subtype is of interest in the pathophysiology and treatment of depression, anxiety, and migraine. Over recent years 5-HT_1B receptor binding in human brain has been examined with PET using radioligands that are partial but not full agonists. To explore how the intrinsic activity of a PET radioligand may affect imaging performance, two high-affinity full 5-HT_1B receptor agonists (AZ11136118, 4; and AZ11895987, 5) were selected from a large compound library and radiolabeled for PET examination in non-human primates.

Methods

[¹¹C]4 was obtained through Pd(0)-mediated insertion of [¹¹C]carbon monoxide between prepared iodoarene and homochiral amine precursors. [¹¹C]5 was obtained through

SUBMITTER: Lindberg A 

PROVIDER: S-EPMC6591083 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature