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

Adrenergic Modulation With Photochromic Ligands

Davia Prischich  1   2 , Alexandre M J Gomila  1   2 , Santiago Milla-Navarro  3 , Gemma Sangüesa  4   5 , Rebeca Diez-Alarcia  6   7 , Beatrice Preda  1 , Carlo Matera  1   2 , Montserrat Batlle  4   5 , Laura Ramírez  3 , Ernest Giralt  8   9 , Jordi Hernando  10 , Eduard Guasch  4   5 , J Javier Meana  6   7 , Pedro de la Villa  3   11 , Pau Gorostiza  1   2   12
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Free article

Adrenergic Modulation With Photochromic Ligands

Davia Prischich et al. Angew Chem Int Ed Engl. .
Free article

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.

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