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.

Adrenergic modulation with photochromic ligands / D. Prischich, A.M.J. Gomila, S. Milla-Navarro, G. Sangüesa, R. Diez-Alarcia, B. Preda, C. Matera, M. Batlle, L. Ramírez, E. Giralt, J. Hernando, E. Guasch, J.J. Meana, P. de la Villa, P. Gorostiza. - In: ANGEWANDTE CHEMIE. INTERNATIONAL EDITION. - ISSN 1433-7851. - 60:7(2021), pp. 3625-3631. [10.1002/anie.202010553]

Adrenergic modulation with photochromic ligands

C. Matera;
2021

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.
adrenergic receptors; azo compounds; neurotransmitters; photochromism; photopharmacology
Settore CHIM/08 - Chimica Farmaceutica
Settore BIO/14 - Farmacologia
2020
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/778579
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