Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion

Several, if not all adrenergic β-blockers (β-Bs), accumulate progressively inside secretory vesicles in a time- and concentration-dependent manner, and could be considered to be false neurotransmitters. This transmitter effect is most likely unrelated to their ability to block adrenergic receptors,...

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Autores principales: Beltran, Beatriz, Carrillo, Romen, Martin, Tomas, Martin, Victor S., Machado, Jose D., Borges, Ricardo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2011
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4055874/
https://www.ncbi.nlm.nih.gov/pubmed/26791642
http://dx.doi.org/10.3390/ph4050713
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author Beltran, Beatriz
Carrillo, Romen
Martin, Tomas
Martin, Victor S.
Machado, Jose D.
Borges, Ricardo
author_facet Beltran, Beatriz
Carrillo, Romen
Martin, Tomas
Martin, Victor S.
Machado, Jose D.
Borges, Ricardo
author_sort Beltran, Beatriz
collection PubMed
description Several, if not all adrenergic β-blockers (β-Bs), accumulate progressively inside secretory vesicles in a time- and concentration-dependent manner, and could be considered to be false neurotransmitters. This transmitter effect is most likely unrelated to their ability to block adrenergic receptors, but it could explain the delay in lowering arterial pressure in hypertensive patients. We have developed a new drug to monitor the accumulation of β-Bs inside living cells, RCTM-3, which fluoresces in the visible spectrum. Here we describe the procedure to synthesize this new compound, as well as its fluorescent properties, pharmacological profile and its accumulation inside the secretory vesicles of PC12 cells.
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spelling pubmed-40558742014-06-13 Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion Beltran, Beatriz Carrillo, Romen Martin, Tomas Martin, Victor S. Machado, Jose D. Borges, Ricardo Pharmaceuticals (Basel) Article Several, if not all adrenergic β-blockers (β-Bs), accumulate progressively inside secretory vesicles in a time- and concentration-dependent manner, and could be considered to be false neurotransmitters. This transmitter effect is most likely unrelated to their ability to block adrenergic receptors, but it could explain the delay in lowering arterial pressure in hypertensive patients. We have developed a new drug to monitor the accumulation of β-Bs inside living cells, RCTM-3, which fluoresces in the visible spectrum. Here we describe the procedure to synthesize this new compound, as well as its fluorescent properties, pharmacological profile and its accumulation inside the secretory vesicles of PC12 cells. MDPI 2011-04-28 /pmc/articles/PMC4055874/ /pubmed/26791642 http://dx.doi.org/10.3390/ph4050713 Text en © 2011 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Beltran, Beatriz
Carrillo, Romen
Martin, Tomas
Martin, Victor S.
Machado, Jose D.
Borges, Ricardo
Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion
title Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion
title_full Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion
title_fullStr Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion
title_full_unstemmed Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion
title_short Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion
title_sort fluorescent β-blockers as tools to study presynaptic mechanisms of neurosecretion
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4055874/
https://www.ncbi.nlm.nih.gov/pubmed/26791642
http://dx.doi.org/10.3390/ph4050713
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