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

Autor: Jose D. Machado, Beatriz Beltran, Romen Carrillo, Tomas Martin, Victor S. Martin, Ricardo Borges
Jazyk: angličtina
Rok vydání: 2011
Předmět:
Zdroj: Pharmaceuticals, Vol 4, Iss 5, Pp 713-725 (2011)
Druh dokumentu: article
ISSN: 1424-8247
DOI: 10.3390/ph4050713
Popis: 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.
Databáze: Directory of Open Access Journals