Mydriasis elicited by imidazol(in)e α2-adrenomimetics in comparison with other adrenoceptor-mediated effects and hydrophobicity

Nasal, Antoni; Frąckowiak, Teresa; Petrusewicz, Jacek; Buciński, Adam; Kaliszan, Roman

doi:10.1016/0014-2999(94)00721-i

Cited by 5 publications

(2 citation statements)

References 35 publications

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“…First, the pK a value of brimonidine is 7.78, yielding an aqueous solution with an approximately neutral pH. Second, the logP value of brimonidine is 0.83, which is similar to the logP of clonidine (0.73) used for mucosally administered general sedation [ 23 ]. In contrast, the logP value of dexmedetomidine, which exhibits high permeability and low solubility that limit bioavailability for local administration, is 3.44 [ 24 ].…”

Section: Discussionmentioning

confidence: 99%

Preliminary evaluation of the efficacy and safety of brimonidine for general anesthesia

et al. 2021

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Background To determine the hypnotic and analgesic effects of brimonidine, and evaluate its efficacy and safety for general anesthesia. Potentiation of pentobarbital sleeping time following brimonidine administration was observed in mice, as was the analgesic activity of brimonidine. Methods The median effective dose (ED50) and lethal dose (LD50) of intraperitoneally injected brimonidine were determined in hypnotized mice. In addition, the LD50 of intravenously injected brimonidine, and ED50 of intravenously, intramuscularly, and intrarectally injected brimonidine in hypnotized rabbits were determined. Finally, the synergistic anesthetic effect of brimonidine and chloral hydrate was evaluated in rabbits. Results Intraperitoneal injection of 10 mg/kg brimonidine enhanced the hypnotic effect of a threshold dose of pentobarbital. Intraperitoneally injected brimonidine produced dose-related analgesic effects in mice. The ED50 of intraperitoneally administered brimonidine in hypnotized mice was 75.7 mg/kg and the LD50 was 379 mg/kg. ED50 values of intravenous, intramuscular, and intrarectal brimonidine for hypnosis in rabbits were 5.2 mg/kg, 8.8 mg/kg, and 8.7 mg/kg, respectively; the LD50 of intravenous brimonidine was 146 mg/kg. Combined intravenous administration of 0.6 mg/kg brimonidine and 0.03 g/kg chloral hydrate had a synergistic anesthetic effect. Conclusions Brimonidine elicited hypnotic and analgesic effects after systemic administration and exhibited safety. Moreover, brimonidine enhanced the effects of other types of narcotics when combined.

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Section: Discussionmentioning

confidence: 99%

Preliminary evaluation of the efficacy and safety of brimonidine for general anesthesia

et al. 2021

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“…First, halogen substitution increases the lipophilicity of a molecule, thus improving its absorption and its permeability to the blood brain barrier or the blood ocular barrier 12 . This property is correlated with the potency of hypotensive agents acting on the central nervous system (CNS) 13,14 . Moreover, lipophilic substitutions at the positions 2 and 6 of the phenyl ring are well tolerated in terms of pharmacological activity both by α1-and α2-ARs 15 .…”

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confidence: 99%

Adrenergic Modulation With Photochromic Ligands

et al. 2020

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Adrenoceptors are ubiquitous and regulate heart and respiratory rate, digestion, metabolism, and vascular tone. They can be activated or blocked with adrenergic drugs, but systemic administration causes broad adverse effects. We have developed photochromic ligands (adrenoswitches) to switch on and off adrenoceptor activity on demand at selected locations. Their pharmacology, photochromism, bioavailability and lack of toxicity allow photomodulating adrenergic signalling, as demonstrated by controlling locomotion in zebrafish and pupillary responses in blind mice. File list (2) download file view on ChemRxiv Adrenergic modulation with photochromic ligands (main ... (573.43 KiB) download file view on ChemRxiv Adrenergic modulation with photochromic ligands (SI).pdf (2.41 MiB)

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Rat clonidine mydriasis model: imidazoline receptors are not involved

Yu¹,

Koss²

2005

Autonomic Neuroscience

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Mydriasis elicited by imidazol(in)e α2-adrenomimetics in comparison with other adrenoceptor-mediated effects and hydrophobicity

Cited by 5 publications

References 35 publications

Preliminary evaluation of the efficacy and safety of brimonidine for general anesthesia

Preliminary evaluation of the efficacy and safety of brimonidine for general anesthesia

Adrenergic Modulation With Photochromic Ligands

Rat clonidine mydriasis model: imidazoline receptors are not involved

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