Adrenergic Modulation With Photochromic Ligands

Angew Chem Int Ed Engl. 2021 Feb 15;60(7):3625-3631. doi: 10.1002/anie.202010553. Epub 2020 Dec 21.

Abstract

Adrenoceptors are ubiquitous and mediate important autonomic functions as well as modulating arousal, cognition, and pain on a central level. Understanding these physiological processes and their underlying neural circuits requires manipulating adrenergic neurotransmission with high spatio-temporal precision. Here we present a first generation of photochromic ligands (adrenoswitches) obtained via azologization of a class of cyclic amidines related to the known ligand clonidine. Their pharmacology, photochromism, bioavailability, and lack of toxicity allow for broad biological applications, as demonstrated by controlling locomotion in zebrafish and pupillary responses in mice.

Keywords: adrenergic receptors; azo compounds; neurotransmitters; photochromism; photopharmacology.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic Agents / chemical synthesis
  • Adrenergic Agents / chemistry
  • Adrenergic Agents / pharmacology*
  • Animals
  • Chromogenic Compounds / chemical synthesis
  • Chromogenic Compounds / chemistry
  • Chromogenic Compounds / pharmacology*
  • Ligands
  • Mice
  • Mice, Nude
  • Molecular Structure
  • Receptors, Adrenergic / metabolism*
  • Zebrafish

Substances

  • Adrenergic Agents
  • Chromogenic Compounds
  • Ligands
  • Receptors, Adrenergic