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Adrenergic Modulation With Photochromic Ligands
Author(s) -
Prischich Davia,
Gomila Alexandre M. J.,
MillaNavarro Santiago,
Sangüesa Gemma,
DiezAlarcia Rebeca,
Preda Beatrice,
Matera Carlo,
Batlle Montserrat,
Ramírez Laura,
Giralt Ernest,
Hernando Jordi,
Guasch Eduard,
Meana J. Javier,
Villa Pedro,
Gorostiza Pau
Publication year - 2021
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.202010553
Subject(s) - photochromism , zebrafish , clonidine , adrenergic , neuroscience , arousal , chemistry , neurotransmission , adrenergic receptor , ligand (biochemistry) , receptor , biology , endocrinology , biochemistry , photochemistry , gene
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.