著者

小島 正美

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.132, no.5, pp.555-559, 2012

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A lot of healthcare professionals experienced annoyance with biased mass media news regarding medical and health issues. In this paper, I propose "news profiling method" and "media guideline" to improve the medical and health journalism.<br>

著者

杉本 八郎 山西 嘉晴 小倉 博雄 飯村 洋一 山津 清實

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.119, no.2, pp.101-113, 1999-02-01 (Released:2008-05-30)

参考文献数

28

被引用文献数

3 9

---

The most consistent change of neurotransmitter in the brain of Alzheimer's patients is the dramatic decrease of cholinergic innervation due to the loss of neurons in the basal forebrain. The most widely studied acetylcholinesterase inhibitors (AChEIs) have been physostigmine and tacrine. Physostigmine has very short duration, and tacrine has liability to hepatotoxicity. These are the defects of the inhibitors. Our objective was to find a new type of AChEIs that would overcome the disadvantages of physostigmine and tacrine. Through a random screening, we incidentally found an N-benzylpiperazine derivative which showed positive cholinergic behavior in rats. We replaced the N-benzylpiperazine moiety with N-benzylpiperidine moiety and found a dramatic increase in anti-AChE activity. Even after the replacement of an amide group with a ketone group the activity was held. Furthermore, the cyclic-amide derivative showed enhanced inhibitory activity. On the basis of these results, an indanone derivative was designed. Among these indanone derivatives, donepazil hydrochloride (E2020), brand name ARICEPT was found to be the most balanced compound. The clinical studies of donepezil hydrochloride demonstrated statistically significant effects on ADAS-cog (Alzheimer's Disease Assessment Scale cognitive sub.) and CIBIC Plus (Clinician's Interview-Based Impression of Change plus).

著者

谷村 顕雄 秦 邦男 竹下 隆三

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.84, no.7, pp.652-655, 1964-07-25 (Released:2010-02-19)

参考文献数

11

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Analysis was made on the composition of torula yeast, prepared from sulfite pulp waste liquor, using Torulopsis utilis, in order to elucidate the factor accelerating animal growth. Ethanol extract of torula yeast was fractionated and examination was made on several crystalline substances obtained. Besides D-galactose, ergosterol, and myristic acid, 1, 2, 3, 5, 6-penta-O-acetyl-α-D-galactofuranose was obtained in 0.11% yield. This is the first example of its presence in a natural product and it is interesting that a substance with so many acetyl groups had been found in nature.

著者

芝 清隆

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.129, no.11, pp.1295-1302, 2009 (Released:2009-11-01)

参考文献数

26

被引用文献数

1 1

---

Motif-programming is a method for creating artificial proteins by combining functional peptide motifs in a combinatorial manner. Motifs are often short amino acid sequences within natural proteins that are associated with particular biological functions. Motifs also can be created de novo using molecular engineering. In particular, peptide aptamers, which have been isolated as specific binders against various targets, are believed to be promising motif blocks for creating novel biomaterials through motif-programming. It is now known, however, that simple arithmetic addition does not always work with motif-programming-e.g., simple conjugation of motifs-A and -B does not always result in a bifunctional peptide-AB. To solve this nonlinearity in motif-programming, we have been employing a combinatorial approach, which we called MolCraft. In MolCraft, we prepare a library of artificial proteins that contain multiple motifs in various numbers and orders, from which clones having the desired functions are selected. In MolCraft, a microgene is first rationally designed so that the encoded peptides contain motifs, and then tandemly polymerized with insertion or deletion mutations at the junctions between microgene units. Because of junctional perturbations, proteins translated from a single microgene polymer are molecularly diverse, originating from the combinatorics of three reading frames, and are thus combinatorial polymers of three peptides. By embedding functional motifs into different reading frames of a single microgene, combinatorial polymers of functional motifs are easily prepared. Notably, repetitiousness retained in the overall structure of proteins contributes to the formation of ordered structures, and enhances the chances of reconstituting biological activity. This method is particularly well suited for developing liaison molecules that interface between cells and inorganic materials. Examples of multifunctional artificial proteins created from this method will be introduced.

著者

谷内 信彦 新留 徹広 杉本 八郎

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.135, no.2, pp.323-329, 2015-02-01 (Released:2015-02-01)

参考文献数

36

被引用文献数

1 1

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In addition to cognitive decline, Alzheimer's disease patients also exhibit non-cognitive symptoms commonly referred to as behavioral and psychological symptoms of dementia, or BPSD. These symptoms have a serious impact on the quality of life of these patients, as well as that of their caregivers, but there are currently no effective therapies. The amyloid β-peptide (Aβ) is suspected to play a central role in the cascade leading to Alzheimer's disease, but the precise mechanisms are still incompletely known. To assess the influence of Aβ pathology on cognitive and non-cognitive behaviors, we examined locomotor activity, motor coordination, and spatial memory in male and female APPswePS1dE9 mice (Alzheimer's disease model, double transgenic mice expressing an amyloid precursor protein with Swedish mutation and a presenilin-1 with deletion of exon 9) at 5 months of age, when the mice had subtle Aβ deposits, and again at 9 months of age, when the mice had numerous Aβ deposits. Compared to wild-type mice, the male and female APPswe/PS1dE9 mice showed normal motor coordination in the rotarod test at both 5 and 9 months. In the Morris water maze test, male and female APPswe/PS1dE9 mice showed impaired spatial memory at 9 months; however, no such deficits were found at 5 months. In a locomotor activity test, male APPswe/PS1dE9 mice exhibited locomotor hyperactivity at 9 months, while females exhibited locomotor hyperactivity at both 5 and 9 months compared to the control mice. Together, these results indicate that APPswe/PS1dE9 mice developed spatial memory impairment and BPSD-like behavioral alterations resulting from Aβ accumulation.

著者

古瀬 幹夫

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.134, no.5, pp.615-621, 2014 (Released:2014-05-01)

参考文献数

13

被引用文献数

1

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Within an epithelial cellular sheet, the paracellular pathway can be divided into two routes: one between two adjacent cells and one at tricellular contacts, where the vertices of three cells meet. For epithelial barrier function, tight junctions restrict solute permeability through the paracellular pathway between two cells, while tricellular contacts contain specialized structures of tight junctions, named tricellular tight junctions (tTJs). Two types of membrane proteins, tricellulin and angulin family proteins (angulin-1/LSR, angulin-2/ILDR1 and angulin-3/ILDR2) have been identified as molecular components of tTJs. Angulins recruit triellulin to tTJs and these tTJ-associated proteins are required for normal tTJ formation as well as strong epithelial barrier function. Furthermore, mutations in tricellulin and angulin-2/ILDR1 genes cause autosomal recessive familial deafness, DFNB49 and DFNB42, respectively. Further analyses of the angulin-tricellulin system should lead to better understanding of the molecular mechanism and regulation of tTJs.

著者

飯嶋 久志 大澄 朋香 小清水 敏昌

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.130, no.9, pp.1215-1223, 2010 (Released:2010-09-01)

参考文献数

71

被引用文献数

2 2

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In recent years, Evidence-based Medicine is practiced in medical care, and meta-analysis is positioned as the highest quality research paper. However, there are no unified criteria to evaluate meta-analysis. Thus, we developed and evaluated objective criteria of meta-analysis paper. Meta-analysis was evaluated from the standpoint of format and quality. Format score was developed based on QUOROM statement. Quality scores were evaluated in each step of meta-analysis. We evaluated meta-analysis for advantageous or adverse effect in the relationship between Renin-angiotensin system (RAS) inhibitor and diabetes mellitus. Research articles either in English or Japanese were searched in PubMed and the Cochrane Library in July 2009. Fifty-five studies were evaluated for format and quality score. Format score was 64.5±25.3% (Mean±S.D.), and quality score was 57.1±21.6%. After plotting each score along the X-Y coordinate, format score was correlated with quality score (R2=0.702, p<0.001). In studies with quality score of 70% or higher, RAS inhibitor prevented new-onset diabetes mellitus. Angiotensin converting enzyme (ACE) inhibitor reduced risk of myocardial infarction, however, angiotensin receptor blockers (ARB) increased the incidence in odds ratio 1.21 (95%CI: 1.04-1.40). We evaluated meta-analysis by format and quality score, and these factors showed correlation. Therefore, assessment of quality score leads to prompt and reliable evaluation of meta-analysis. According to articles evaluated by quality score, RAS inhibitor showed effectiveness on diabetes mellitus. However, careful attention must be given in ARB therapy on patients with myocardial infarction risk.

著者

濱口 常男 鎌田 彩 村岡 玲子 倉本 美佳 中元 智子 志方 敏幸 門林 宗男

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.125, no.6, pp.525-530, 2005-06-01 (Released:2005-06-01)

参考文献数

8

被引用文献数

2 3

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For the purpose of quality evaluation of magnesium oxide (MgO) tablets, we considered the dissolution test method with changes in the pH of the dissolution medium as an indicator and studied the elution behavior of MgO from commercial MgO tablets. We also studied the effects of particle size on the elution rate of MgO from MgO tablets. A dissolution test was carried out using the rotating basket method in 100 ml of the first fluid (pH 1.2). The stirring speed was set at 200 rpm. The elution behaviors of MgO from two products were markedly different. The medium pH for the sample MM (Magmit) tablet after 15 min reached 9.5 but that for ML (Maglax) tablet was 2.7 even after 60 min. The apparent solubility of MgO in 100 ml of the first fluid were, respectively, 175 mg and 100 mg when medium pH as 9.5 and 1.5. The low dissolution of ML tablets is thought to be due to the large particle size (average particle size r = 226 μm) or due to the effects of additives on elution. These results suggest that neutralizing activity after ingestion of MgO tablets and subsequent laxative effects may, when conditions after ingestion of MM tablets and after ingestion of ML tablets are compared, produce differences between them. We found that the dissolution test method with pH as an indicator is useful in assessing the dissolution behavior of MgO preparations.

著者

渡邉 文之 篠原 久仁子 土橋 朗 天貝 賢二 原 和夫 倉田 香織 飯嶋 秀郎 島川 清 島田 匡彦 阿部 櫻子 武井 敬司 亀井 美和子

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI

巻号頁・発行日

vol.136, no.9, pp.1243-1254, 2016

被引用文献数

3

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&emsp;This study built a protocol for drug therapy management (hereinafter &ldquo;the protocol&rdquo;) that would enable continuous support from the decision making of smoking cessation therapy to the completion of therapy through the collaboration of physicians and community pharmacists, after which we evaluated whether the use of this protocol would be helpful to smoking cessation therapy. This study utilized the &ldquo;On the Promotion of Team-Based Medical Care&rdquo;, a Notification by the Health Policy Bureau as one of the resources for judgment, and referred to collaborative drug therapy management (CDTM) in the United States. After the implementation of this protocol, the success rate of smoking cessation at the participating medical institutions rose to approximately 70%, approximately 28-point improvement compared to the rate before the implementation. In addition to the benefits of the standard smoking cessation program, this result may have been affected by the intervention of pharmacists, who assisted in continuing cessation by advising to reduce drug dosage as necessary approximately one week after the smoking cessation, when side effects and the urge to smoke tend to occur. Additionally, the awareness survey for the intervention group revealed that all respondents, including patients who failed to quit smoking, answered that they were satisfied to the question on general satisfaction. The question about the reason for successful cessation revealed that the support by pharmacists was as important as, or more important than, that by physicians and nurses. This infers that the pharmacists' active engagement in drug therapy for individual patients was favorably acknowledged.<br>

著者

長井 紀章

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.136, no.10, pp.1385-1390, 2016 (Released:2016-10-01)

参考文献数

20

被引用文献数

5

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The ophthalmic application of drugs is the primary route of administration for the therapy of glaucoma; however, in traditional formulations, only small amounts of the administered drug penetrate the cornea to reach the desired intraocular tissue due to corneal barriers. Recently, nanoparticulate drug delivery is expected as a technology to overcome the difficulties in delivering drugs across biological barriers (improvement of bioavailability). In this study, we attempted to establish a new method for preparing solid drug nanoparticles by using a bead mill and various additives, and succeeded in preparing a high quality dispersion containing drug nanoparticles. For a more concrete example, a mean particle size of disulfiram (DSF) treated with bead mill is 183 nm. The corneal penetration and corneal residence time of DSF from the ophthalmic dispersion containing DSF nanoparticles were significantly higher than those from a 2-hydroxypropyl-β-cyclodextrin solution containing DSF (DSF solution). It is known that the administration of DSF has intraocular pressure (IOP)-reducing effects. The IOP-reducing effects of the ophthalmic dispersion containing DSF nanoparticles were significantly greater than those of the DSF solution in rabbits (the IOP was enhanced by placing the rabbits in a dark room for 5 h). In addition, the ophthalmic dispersion containing DSF nanoparticles is better tolerated by corneal epithelial cells than DSF solution. It is possible that dispersions containing DSF nanoparticles provide new possibilities for effectively treating glaucoma, and that ocular drug delivery systems using drug nanoparticles may expand their usage for therapy in the ophthalmologic field.

著者

島野 仁

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.135, no.9, pp.1003-1009, 2015 (Released:2015-09-01)

参考文献数

17

被引用文献数

4

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Recent studies suggest that chronic local inflammation and cellular stresses are the key steps in organ defects in obesity-related diseases such as atherosclerosis, diabetes, and fatty liver. We have shown that an excess energy state activates sterol regulatory element-binding protein (SREBP)-1c, a master transcription factor for fatty acid synthesis causing the accumulation of lipids leading to fatty liver, insulin resistance, insulin secretion defects, and dyslipidemia and we clarified their molecular mechanisms. Recently, we shifted focus to the quality aspect of accumulated lipids. It has long been known that saturated and poly-unsaturated fatty acids are atherogenic and anti-atherogenic, respectively. Besides desaturation, we found that the chain-length of fatty acids is another important factor. Elovl6 that we have cloned as an SREBP-1 target is a fatty acid elongase that catalises the last step of fatty acid synthesis. Elovl6 KO mice exhibit obesity and fatty liver on a high energy diet, but unexpectedly were immune to insulin resistance (Nat. Med., 13, 2007, Matsuzaka et al.), atherosclerosis (Arterioscler. Thromb. Vasc. Biol., 31, 2011, Saito et al.) and non-alcoholic steatohepatitis (NASH) pathology including liver damage, ROS, and fibrosis (Hepatology, 56, 2012, Matsuzaka et al.). Elovl6 is crucial for protection against lung fibrosis (Nat. Commun., 4, 2013, Sunaga et al.). These data implicate that fatty acid composition is a new therapeutic target for a variety of chronic metabolic diseases. In this symposium review, a novel strategy for the prevention of life-related diseases will be discussed in the standpoint of application of wet-dry fusion strategies for theoretical and medicinal chemistry.

著者

川田 稔 高梨 茂 中島 靖夫

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.774-776, 1961-05-25 (Released:2010-02-19)

参考文献数

4

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Ferrous [59Fe] D-glucuronate was prepared from glucuronic acid and ferrous [59Fe] carbonate which was obtained from 59FeCl3. In this reaction almost the whole process was carried out automatically in nitrogen atmosphere. Determination of glucuronic acid in ferrous glucuronate by naphthoresorcinol picrate was not disturbed by the presence of radioactive ferrous ion.

著者

綾田 渙

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.778-783, 1961-05-25 (Released:2010-02-19)

参考文献数

11

被引用文献数

1

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Resolution of dl-(2-hydroxy-3-cyanopropyl) trimethylammonium chloride (III) was carried out with d-tartaric acid or dibenzoyl-d-tartaric acid, and dextro- and levorotatory compounds of (III) were obtained. Hydrolysis of these optically active (III) with conc. hydrochloric acid by heating in a boiling water bath afforded the corresponding d- and l-(2-hydroxy-3-carboxypropyl) trimethylammonium chloride (VII). Of these, the levorotatory (VII) was found to correspond to the hydrochloride of natural carnitine (VIII). Infrared spectra of these compounds are given.

著者

市川 正孝 高木 康 一番ケ瀬 尚

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.768-771, 1961-05-25 (Released:2010-02-19)

参考文献数

4

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Nitration of ethyl 8-hydroxycoumarin-3-carboxylate (I) in glacial acetic acid solution affords ethyl 5-nitro-8-hydroxycoumari-3-carboxylate (III), m.p. 203.5-204°, and ethyl 7-nitro-8-hydroxycoumarin-3-carboxylate (IV), m.p. 201-202°. Methylation of (III) and (IV) with methyl iodide respectively gives 8-methoxy compounds, (VII) of m.p. 184-186°, and (VIII) of m.p. 152°, respectively. On the other hand, nitration of 3-methoxy-salicylaldehyde acetate (XVI) affords 4-nitro (IX), m.p. 92-93°, 5-nitro (X), m.p. 142°, and 6-nitro (XI), m.p. 104°, compounds. By condensation of (IX) and (XI) with ethyl malonate, in the presence of piperidine, the position of the nitro group in the foregoing (III) and (IV) was determined.Hydrolysis of (I), (III), and (IV) with hydrochloric acid respectively afforded 8-hydroxycoumarin-3-carboxylic acid, m.p. 292-293° (decomp.), 5-nitro-8-hydroxycoumarin-3-carboxylic acid, m.p. 292-293° (decomp.), 5-nitro-8-hydroxycoumarin-3-carboxylic acid (V), 257-258°, and 7-nitro-8-hydroxycoumarin-3-carboxylic acid (VI), m.p. 246-248°.

著者

桑野 晴光 田村 千尋

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.764-767, 1961-05-25 (Released:2010-02-19)

参考文献数

5

被引用文献数

2 2

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Polymorphism of chloramphenicol was examined by the X-ray diffraction method and quantitative relationship between the two crystal forms was examined. In general, proportionation of concentration to diffraction intensity can be quantitated in polymorphs but the method was inconvenient for use with organic compounds due to strict packing conditions. In the binary system (α- and β-forms) of chloramphenicol palmitate, specific intensity and specific concentration of the component were in proportion and quantitative straight line independent of packing codition was obtained. This was found to be effective in the range of over 3% of the β-form and precision is within 1%. As the quantitative linear equation: the following was obtained: xβ/xα=(0.347±0.005)⋅Iβ/Iα, where x is the concentration of the component and I is the intensity of reflection.

著者

田村 千尋 桑野 晴光

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.759-764, 1961-05-25 (Released:2010-02-19)

参考文献数

6

被引用文献数

1 1

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From the consideration of X-ray diffraction, infrared absorption spectra, and various transition conditions of long-chain esters of chloramphenicol, and some assumptions were made on their crystal structure.1) According to X-ray diffraction, all-trans configuration for the long-chain portion of the β-form molecule results in good agreement between the molecular models and the long axis by X-ray measurement. In the case of α-form, the long axis of the crystal cannot be explained unless the molecule is assumed to have some cis linkages or the long chain part is a trans structure but deeply twined with each other.2) Infrared absorption spectra suggest that the α-form is closely resembled to a solution state and crystals with a cis configuration, having distorted molecule, may be assumed. The β-form is considered to have a higher order molecular arrangement as a crystal and it is convenient to assume an all-trans configuration by X-ray measurement.3) Stability of the β-form can be assumed form the measurement of melting point and specific gravity. On the other hand, similarity to the α-form and solution state (or amorphous state) as found from transition conditions and these agree well with the above two measurements.

著者

田村 千尋 桑野 晴光

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.755-759, 1961-05-25 (Released:2010-02-19)

参考文献数

6

被引用文献数

13 19

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It was found that chloramphenicol palmitate, myristate, and caprylate come in two kinds of crystalline form and one amorphous form. These compounds were prepared and their transition conditions were examined.1) When the crystals is dissolved in a solvent and crystallized out, optional form of crystals can be obtained by controlling crystallization rate and this form is not affected by polarity or pH of the solvent. Crystals of α-form is obtained by rapid crystallization while the β-form is obtained by gradual crystallization. When a small amount is fused and cooled rapidly in a refrigerator, a vitrious substance is obtained.2) Transition between the solids occur only in the direction of amorphous to α-form to β-form, and there is no reverse progress. The transition rate is faster, the nearer the melting point. The mechanism of such a transition is thought to be the transition to a stable form by the heat motion of the molecule itself. The transition rate becomes suddenly rapid after formation of β-form crystal and this is considered to be due to added effect of catalytic transition.

著者

関口 慶二

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.664-669, 1961-05-25 (Released:2010-02-19)

参考文献数

9

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Solubilizing action of the sodium salt of benzoic acid, o-, m-, and p-hydroxy-, methoxy-, amino-, nitro-, and chloro-benzoic acid, and nicotinic acid on caffeine was determined and the effect of the kind and position on the solubilization was examined. The solubilizing action was found to be in the descending order, in molar equivalent of the salt, of salicylate≅m-chloro-, p-chloro-, m-hydroxy-≅p-hydroxy-≅m-methoxy-≅p-methoxy-, m-nitro-, p-nitro-, o-amino-, and p-amino-benzoate, benzoate, m-aminobenzoate, nicotinate, and o-chloro-, o-methoxy-, and o-nitro-benzoate. The solubilizing action of these benzoates is assumed to be not due to formation of a complex of established composition but due to the formation of a hydrogen bond between caffeine and benzoate, with the water molecule of the solvent acting as the hydrogen-bond donor.

著者

掛見 喜一郎 有田 隆一 大橋 貞

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.748-750, 1961-05-25 (Released:2010-02-19)

参考文献数

2

被引用文献数

1 1

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Potency determination of kanamycin solution was carried out as follows: To 5cc. of kanamycin solution in water, 0.5cc. of 20% sodium carbonate solution is added, followed by 0.5cc. of 1% solution of sodium 1, 2-naphthoquinone-4-sulfonate with cooling in ice water, and the mixture is allowed to stand at 0° to 2° for 20 minutes, protected from light. To this solution, 1.0cc. of acetone and 0.5cc. of 50% acetic acid are added and optical density of this solution, is measured at 420 mμ. As a control, the same procedure is carried out with distilled water in place of the sample solution. The potency of the sample solution is read from the calibration curve prepared with kanamycin of known potency.The same determination was carried on samples boiled with acid or alkali, and samples left at various temperatures. Comparison of the values so obtained with the values determined by the cup method, stipulated in the antibiotics standard, showed good agreement.

著者

加瀬 佳年 由井薗 倫一

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.81, no.5, pp.740-747, 1961-05-25 (Released:2010-02-19)

参考文献数

30

被引用文献数

3

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The pharmacology of d-N, N, 1-trimethyl-3-(ethylsulfonyl)-3, 3-diphenylpropylamine hydrochloride (A-5) was described in detail. A-5 showed a long-acting antitussive activity, duration of the effect being 18.9 times that of codeine (intravenous) and 13.5 times that of codeine (oral), though 50% antitussive dose is only 1.4 and 1.7 times that of codeine in dogs and cats, respectively. The site of action seemed to be the cough center per se. Toxicity in mice (subcutaneous) is 1.5 times that of codeine and 30% that of Methadone. No tendency to establish tolerance, cumulative action, or addiction liability was found by long-term administration. Analgesic action and other actions were discussed.