title: Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion.
abstract: 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.
authors.affiliation: Institute of BioOrganic "Antonio Gonzalez", University of La Laguna, La Laguna 38071, Tenerife, Spain. bbeltran@ull.es.
authors.forename: Beatriz
authors.initials: B
authors.lastname: Beltran
authors.affiliation: Institute de Natural Products and Agrobiology, Spanish National Research Council (CSIC), La Laguna 38071, Tenerife, Spain. rcarrillo@ipna.csic.es.
authors.forename: Romen
authors.initials: R
authors.lastname: Carrillo
authors.affiliation: Institute of BioOrganic "Antonio Gonzalez", University of La Laguna, La Laguna 38071, Tenerife, Spain. tmartin@ipna.csic.es.|Institute de Natural Products and Agrobiology, Spanish National Research Council (CSIC), La Laguna 38071, Tenerife, Spain. tmartin@ipna.csic.es.
authors.forename: Tomas
authors.initials: T
authors.lastname: Martin
authors.affiliation: Institute of BioOrganic "Antonio Gonzalez", University of La Laguna, La Laguna 38071, Tenerife, Spain. vmartin@ull.es.
authors.forename: Victor S
authors.initials: VS
authors.lastname: Martin
authors.affiliation: Unit of Pharmacology, Medical School, University of La Laguna, La Laguna 38071, Tenerife, Spain. jdmacha@ull.es.
authors.forename: Jose D
authors.initials: JD
authors.lastname: Machado
authors.affiliation: Institute of BioOrganic "Antonio Gonzalez", University of La Laguna, La Laguna 38071, Tenerife, Spain. rborges@ull.es.|Unit of Pharmacology, Medical School, University of La Laguna, La Laguna 38071, Tenerife, Spain. rborges@ull.es.
authors.forename: Ricardo
authors.initials: R
authors.lastname: Borges
keywords: TIRF; exocytosis; false neurotransmitter; secretory vesicle