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,...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2011-04-01
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| Series: | Pharmaceuticals |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1424-8247/4/5/713/ |
| _version_ | 1811206469621645312 |
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| author | Jose D. Machado Beatriz Beltran Romen Carrillo Tomas Martin Victor S. Martin Ricardo Borges |
| author_facet | Jose D. Machado Beatriz Beltran Romen Carrillo Tomas Martin Victor S. Martin Ricardo Borges |
| author_sort | Jose D. Machado |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-04-12T03:49:09Z |
| format | Article |
| id | doaj.art-ef7bfc45853f490ca5a53d991fb1f614 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-04-12T03:49:09Z |
| publishDate | 2011-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-ef7bfc45853f490ca5a53d991fb1f6142022-12-22T03:49:03ZengMDPI AGPharmaceuticals1424-82472011-04-014571372510.3390/ph4050713Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of NeurosecretionJose D. MachadoBeatriz BeltranRomen CarrilloTomas MartinVictor S. MartinRicardo BorgesSeveral, 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.http://www.mdpi.com/1424-8247/4/5/713/exocytosisfalse neurotransmittersecretory vesicleTIRF |
| spellingShingle | Jose D. Machado Beatriz Beltran Romen Carrillo Tomas Martin Victor S. Martin Ricardo Borges Fluorescent β-Blockers as Tools to Study Presynaptic Mechanisms of Neurosecretion Pharmaceuticals exocytosis false neurotransmitter secretory vesicle TIRF |
| 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 | exocytosis false neurotransmitter secretory vesicle TIRF |
| url | http://www.mdpi.com/1424-8247/4/5/713/ |
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