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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/12/18 12:09:42」(JST)
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English Journal
- Acetazolamide attenuates chemical-stimulated but not thermal-stimulated acute pain in mice.
- Sun YJ1, Chen Y2, Pang C2, Wu N2, Li J2.Author information 11] Department of New Drug Evaluation, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China [2] Now at Beijing Institute of Microbiology and Epidemiology, Beijing 100071, China.2Department of New Drug Evaluation, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.AbstractAim:Acetazolamide (AZA), a carbonic anhydrase (CA) inhibitor, has been found to alleviate inflammatory and neuropathic pain in rats. In the present study, we investigated the effects of AZA on thermal- and chemical-stimulated acute pain in mice and the possible mechanisms underlying the effects.Methods:Five acute pain models based on thermal and chemical stimuli were established to investigate the effects of AZA on different types of nociception in mice. The antinociceptive effects of methazolamide (another CA inhibitor) and diazepam (a positive allosteric modulator of GABAA receptor) were also examined. The drugs were administered either intraperitoneally (ip) or intrathecally.Results:AZA (50-200 mg/kg, ip) did not produce analgesia in two thermal-stimulated acute pain models, ie, mouse tail-flick and hot-plate tests. In contrast, AZA (50-200 mg/kg, ip) dose-dependently reduced paw licking time in both capsaicin and formalin tests in mice. A similar result was observed in a mouse acetic acid-induced writhing test. However, AZA (10 nmol/mouse, intrathecally) did not produce significant analgesia in the 3 chemical-stimulated acute pain models. In addition, methazolamide (50-200 mg/kg, ip) and diazepam (0.25-1.0 mg/kg, ip) did not produce significant analgesia in either thermal- or chemical-stimulated acute pain.Conclusion:AZA produces analgesia in chemical-stimulated, but not thermal-stimulated acute pain in mice. The attenuation of chemical-stimulated acute pain by AZA may not be due to enhancement of GABAA receptor-mediated inhibition via inhibiting CA activity but rather a peripheral ion channel-related mechanism.
- Acta pharmacologica Sinica.Acta Pharmacol Sin.2014 Jan;35(1):41-7. doi: 10.1038/aps.2013.149. Epub 2013 Dec 16.
- Aim:Acetazolamide (AZA), a carbonic anhydrase (CA) inhibitor, has been found to alleviate inflammatory and neuropathic pain in rats. In the present study, we investigated the effects of AZA on thermal- and chemical-stimulated acute pain in mice and the possible mechanisms underlying the effects.Meth
- PMID 24335844
- Sulfonamide inhibition studies of the γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis.
- Vullo D1, Del Prete S2, Osman SM3, De Luca V2, Scozzafava A1, Alothman Z3, Supuran CT4, Capasso C5.Author information 1Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.2Istituto di Biochimica delle Proteine and Institute of Bioscience and Bioresources (IBBR), CNR, Via P. Castellino 111, 80131 Napoli, Italy.3Department of Chemistry, College of Science, King Saud University, PO Box 2455, Riyadh 11451, Saudi Arabia.4Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy; Department of Chemistry, College of Science, King Saud University, PO Box 2455, Riyadh 11451, Saudi Arabia; Università degli Studi di Firenze, Polo Scientifico, Dipartimento NEIROFABA, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Firenze), Italy. Electronic address: claudiu.supuran@unifi.it.5Istituto di Biochimica delle Proteine and Institute of Bioscience and Bioresources (IBBR), CNR, Via P. Castellino 111, 80131 Napoli, Italy. Electronic address: c.capasso@ibp.cnr.it.AbstractA carbonic anhydrase (CA, EC 4.2.1.1) denominated PgiCA, belonging to the γ-class, from the oral pathogenic bacteria Porphyromonas gingivalis, the main causative agent of periodontitis, was investigated for its inhibition profile with sulfonamides and one sulfamate. Dichlorophenamide, topiramate and many simple aromatic/heterocyclic sulfonamides were ineffective as PgiCA inhibitors whereas the best inhibition was observed with halogenosulfanilamides incorporating heavy halogens, 4-hydroxy- and 4-hydroxyalkyl-benzenesulfonamides, acetazolamide, methazolamide, zonisamide, indisulam, celecoxib, saccharin and hydrochlorothiazide (KIs in the range of 131-380nM). The inhibition profile of PgiCA was very different from that of CAM, hCA I and II or the β-CA from a protozoan parasite (Leishmania donovani chagasii). Identification of potent and possibly selective inhibitors of PgiCA may lead to pharmacological tools useful for understanding the physiological role(s) of this enzyme.
- Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2014 Jan 1;24(1):240-4. doi: 10.1016/j.bmcl.2013.11.030. Epub 2013 Nov 21.
- A carbonic anhydrase (CA, EC 4.2.1.1) denominated PgiCA, belonging to the γ-class, from the oral pathogenic bacteria Porphyromonas gingivalis, the main causative agent of periodontitis, was investigated for its inhibition profile with sulfonamides and one sulfamate. Dichlorophenamide, topiramate an
- PMID 24316122
Japanese Journal
- CLINICAL INVESTIGATION : Bilateral transient myopia, angle-closure glaucoma, and choroidal detachment induced by methazolamide
- Kwon Soon Jae,Park Dong Ho,Shin Jae Pil
- Japanese journal of ophthalmology : the official English-language journal of the Japanese Ophthalmological Society 56(5), 515-517, 2012-09
- NAID 40019415455
- Methazolamide Calcium Phosphate Nanoparticles in an Ocular Delivery System
- CHEN Rui,QIAN Yong,LI Rui,ZHANG Qing,LIU Dongfei,WANG Miao,XU Qunwei
- YAKUGAKU ZASSHI 130(3), 419-424, 2010
- … A new system for the local delivery of methazolamide to the eye has been developed based on calcium phosphate (CaP) nanoparticles. … The methazolamide loaded CaP nanoparticles were prepared through the formation of an inorganic core of CaP and further adsorption of the methazolamide. … The maximum loading of methazolamide studied using UV-vis spectrophotometry was about 0.2% (w/w). …
- NAID 130000259524
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