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Pharmaceuticals 2011, 4(5), 713-725; doi:10.3390/ph4050713

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

Institute of BioOrganic “Antonio Gonzalez”, University of La Laguna, La Laguna 38071, Tenerife, Spain
Institute de Natural Products and Agrobiology, Spanish National Research Council (CSIC), La Laguna 38071, Tenerife, Spain
Unit of Pharmacology, Medical School, University of La Laguna, La Laguna 38071, Tenerife, Spain
Author to whom correspondence should be addressed.
Received: 6 April 2011 / Accepted: 20 April 2011 / Published: 28 April 2011
(This article belongs to the Special Issue Betablockers)


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.
Keywords: exocytosis; false neurotransmitter; secretory vesicle; TIRF exocytosis; false neurotransmitter; secretory vesicle; TIRF
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Beltran, B.; Carrillo, R.; Martin, T.; Martin, V.S.; Machado, J.D.; Borges, R. Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion. Pharmaceuticals 2011, 4, 713-725.

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