Highly water-soluble derivatives of the anesthetic agent propofol: in vitro and in vivo evaluation of cyclic amino acid esters.

doi:10.1016/S0928-0987(03)00161-1

Paper

DOI: 10.1016/S0928-0987(03)00161-1

Highly water-soluble derivatives of the anesthetic agent propofol: in vitro and in vivo evaluation of cyclic amino acid esters.

Published Sep 1, 2003 · C. Altomare, G. Trapani, A. Latrofa

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

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Abstract

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In Vitro Study

Study Snapshot

Cyclic amino acid esters of propofol show potential as water-soluble anesthetic agents for parenteral administration, with potential for allosteric modulation of GABA A receptors.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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General Anesthetic Potencies of a Series of Propofol Analogs Correlate with Potency for Potentiation of γ-Aminobutyric Acid (GABA) Current at the GABAA Receptor but Not with Lipid Solubility

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Citations

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Novel piperidine HIV-1 protease inhibitors show improved inhibitory effects and potency against DRV-resistant variants, with potential for designing more potent inhibitors.

2021·14citations·Mei Zhu et al.·European journal of medicinal chemistry

European journal of medicinal chemistry

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Design, Synthesis and Activity Study of a Water-soluble, Rapid-release Propofol Prodrug.

Water-soluble propofol prodrugs with glycolic acid as a linker improve safety, anesthesia onset and duration while maintaining clinical benefits compared to fospropofol.

2020·6citations·Liangming Liu et al.·Journal of medicinal chemistry

Journal of medicinal chemistry

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An improved water‐soluble prodrug of propofol with high molecular utilization and rapid onset of action

HX0921 is an improved propofol prodrug with faster onset of action and shorter anesthesia duration compared to fospropofol, offering benefits for rapid onset and recovery.

2019·6citations·WeiYi Zhang et al.·European Journal of Pharmaceutical Sciences

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Monodisperse oligoethylene glycols modified Propofol prodrugs.

Propofol prodrugs with monodisperse oligoethylene glycols show promise as promising anesthetics for overcoming drawbacks associated with Propofol's low water solubility.

2018·11citations·T. Deng et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

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Amino Acids in the Development of Prodrugs

Amino acids in prodrug design improve bioavailability, decrease toxicity, and target specificity, while preventing fast metabolism and resistance development in therapeutic agents.

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Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry