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Identification of a fluorescent general anesthetic, 1-aminoanthracene.

ABSTRACT: We identified a fluorophore, 1-aminoanthracene (1-AMA), that is anesthetic, potentiates GABAergic transmission, and gives an appropriate dissociation constant, K(d) approximately 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-AMA fluorescence is enhanced when bound to HSAF. Thus, displacement of 1-AMA from HSAF by other anesthetics attenuates the fluorescence signal and allows determination of K(d), as validated by isothermal titration calorimetry. This provides a unique fluorescence assay for compound screening and anesthetic discovery. Additional electrophysiology experiments in isolated cells indicate that 1-AMA potentiates chloride currents elicited by GABA, similar to many general anesthetics. Furthermore, 1-AMA reversibly immobilizes stage 45-50 Xenopus laevis tadpoles (EC(50) = 16 microM) and fluorescence micrographs show 1-AMA localized to brain and olfactory regions. Thus, 1-AMA provides an unprecedented opportunity for studying general anesthetic distribution in vivo at the cellular and subcellular levels.

SUBMITTER: Butts CA

PROVIDER: S-EPMC2672486 | biostudies-literature | 2009 Apr

REPOSITORIES: biostudies-literature

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Identification of a fluorescent general anesthetic, 1-aminoanthracene.

Butts Christopher A CA Xi Jin J Brannigan Grace G Saad Abdalla A AA Venkatachalan Srinivasan P SP Pearce Robert A RA Klein Michael L ML Eckenhoff Roderic G RG Dmochowski Ivan J IJ

Proceedings of the National Academy of Sciences of the United States of America 20090403 16

We identified a fluorophore, 1-aminoanthracene (1-AMA), that is anesthetic, potentiates GABAergic transmission, and gives an appropriate dissociation constant, K(d) approximately 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-AMA fluorescence is enhanced when bound to HSAF. Thus, displacement of 1-AMA from HSAF by other anesthetics attenuates the fluorescence signal and allows determination of K(d), as validated by isothermal titration calorimetry. This ...[more]

PMID: 19346473

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Project description:Surgery patients in Japan undergo routine spirometry testing prior to general anesthesia. The use of a flow sensor during general anesthesia has recently become common. However, it is not certain whether the information derived from flow-volume curves is being adequately used for mechanical ventilation management during general anesthesia. So far, there have been no attempts to calculate airway resistance using flow-volume curves. Therefore, we performed a prospective, observational study to investigate the relationship between pre-anesthetic and intra-anesthetic airway resistance in patients scheduled for surgery under general anesthesia. We calculated pre-anesthetic and intra-anesthetic airway resistance in each patient, based on the slopes of flow-volume curves obtained prior to and during general anesthesia. We also calculated endotracheal tube resistance to correct the intra-anesthetic airway resistance values calculated. A total of 526 patients were included in the study, and 98 patients had a forced expiratory volume in the first second/forced vital capacity ratio of < 70%. Pre-anesthetic airway resistance was significantly higher in patients with airflow obstruction than in those without airflow obstruction (p < 0.001), whereas no significant difference in intra-anesthetic airway resistance was found between patients with and without airflow obstruction during mechanical ventilation (p = 0.48). Pre-anesthetic and intra-anesthetic airway resistance values were closer to each other in patients without airflow obstruction, with a mean difference < 1.0 cmH2O L-1s-1, than in those with airflow obstruction, although these respiratory parameters were significantly different (p < 0.001). Intra-anesthetic airway resistance was not related to the FEV1/FVC ratio, regardless of the degree to which the FEV1/FVC ratio reflected pre-anesthetic airway resistance. As compared with patients with airflow obstruction, the mean difference between pre-anesthetic and intra-anesthetic airway resistance was small in patients without airflow obstruction.

Dataset Information

Identification of a fluorescent general anesthetic, 1-aminoanthracene.

Publications

Identification of a fluorescent general anesthetic, 1-aminoanthracene.

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