著者

城野 久美子 上村 都美子 久野 光造 東出 栄治

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.105, no.8, pp.751-759, 1985-08-25 (Released:2008-05-30)

参考文献数

20

被引用文献数

3 3

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To evaluate the bactericidal activity of antiseptics against many different strains, we devised a modified phenol coefficient method by using microtitration plates based on that of the Association of Analytical chemists, and counted survivors to find the shortest contact time for various concentrations at which almost all bacteria were killed. Benzalkonium chloride (BAC) was bactericidal against all 242 strains tested at 500 μg/ml in 10 min of contact at 25°C. Under the same conditions, chlorhexidine gluconate (CHG) was bactericidal against 90% even at 1000 μg/ml. Among these strains resistant to 1000 μg/ml, Pseudomonas, Serratia, and Proteus species comprised 45% of the strains. The killing rate of BAC was fast, but the bactericidal activity of CHG with short contact time was weaker than its bacteriostatic activity for 24 h. The bactericidal concentration of BAC and CHG for 30 s of contact at 25°C was 500-5000 μg/ml and 5000-30000 μg/ml in a 10% solution of human serum, and 2500->10000 μg/ml and 10000->40000 μg/ml in a suspension of 2.5% dried yeast, respectively. The 10% human serum stimulated the bactericidal activities of BAC and CHG slightly against some test bacteria.

著者

頭金 正博 斎藤 嘉朗

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.5, pp.649-653, 2015-05-01 (Released:2015-05-01)

参考文献数

10

被引用文献数

2 1

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New drug development (NDD) for intractable diseases such as cancer and Alzheimer's disease has been challenging in recent years because it is difficult to evaluate the therapeutic efficacy of new drugs and the response of individual patients. Thus biomarkers might be a useful tool to facilitate NDD because they can be used to evaluate accurately drug responses. Biomarkers include proteins, metabolites, and genetic targets; imaging data and can also be used in pre-clinical studies, clinical trials, and post-marketing surveillance. In pre-clinical studies, biomarkers are used as an index of the pharmacological and toxicological effects of a new drug, which may help to predict the clinical response. In clinical studies, biomarkers are widely used as an index of clinical efficacy and safety for dose-adjustment and for patient selection. In post-clinical studies, biomarkers may facilitate the evaluation of drug responses, as well as aid improvements in drug efficacy. Several points should be considered for biomarker-guided NDD. First, the clinical study design is very important and must be suitable to permit the use of the relevant biomarkers. The analytical methods should be carefully evaluated, and evidence should be provided regarding the physiological significance and relevance of the biomarker with regard to its intended use. Regulatory sciences are required to resolve these issues and bridge the gap between basic science and clinical studies that involve biomarkers.

著者

小西 史朗

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.137, no.4, pp.459-475, 2017-04-01 (Released:2017-04-01)

参考文献数

55

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In the beginning of the 1970s, only two chemical substances, acetylcholine and γ-aminobutyric acid (GABA), had been definitely established as neurotransmitters. Under such circumstances, I started my scientific career in Professor Masanori Otsuka's lab searching for the transmitter of primary sensory neurons. Until 1976, lines of evidence had accumulated indicating that the undecapeptide substance P could be released as a transmitter from primary afferent fibers into spinal synapses, although the substance P-mediated synaptic response had yet to be identified. Peripheral synapses could serve as a good model and thus, it was demonstrated in the prevertebral sympathetic ganglia by1985 that substance P released from axon collaterals of primary sensory neurons acts as the transmitter mediating non-cholinergic slow excitatory postsynaptic potential (EPSP). At that time, we also found that autonomic synapses were useful to uncover the transmitter role of the opioid peptide enkephalins, whose functions had been unknown since their discovery in 1975. Accordingly, enkephalins were found to serve a transmitter role in mediating presynaptic inhibition of cholinergic fast and non-cholinergic slow transmission in the prevertebral sympathetic ganglia. In 1990s, we attempted to devise a combined technique of brain slices and patch-clamp recordings. We applied it to study the regulatory mechanisms that operate around cerebellar GABAergic inhibitory synapses, because most of the studies then had centered on excitatory synapses and because inhibitory synapses are crucially involved in brain functions and disorders. Consequently, we discovered novel forms of heterosynaptic interactions, dual actions of a single transmitter, and receptor crosstalk, the details of which are described in this review.

著者

Toshinari ASAKURA Hiroaki SEINO Seishiro NOZAKI Ryuzo ABE

出版者

The Pharmaceutical Society of Japan

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.121, no.6, pp.459-463, 2001 (Released:2002-09-27)

参考文献数

11

被引用文献数

20 24

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注射針を輸液剤等のゴム栓に穿刺するときに, ゴム栓からゴム片が削り取られるというコアリングが報告されている. 実際に自己注射を行っている患者のインスリンバイアルでもコアリングが発生しているかを確認した. 入院患者30名よりインスリンカートリッジを回収し, 空打ち液, 注入液, カートリッジ残液を試料とした. 発生したゴム片を顕微鏡下で観察し形状と個数, 大きさを測定した. コアリングの発生率は, 空打ち液の発生率は73%, 注入液は47%, カートリッジ残液は97%であった. 形状は, 針を通過している空打ち液と注入液では塊状が多く, 針を通過していないカートリッジ残液では針状が多かった. 空打ち液と注入液では小さなゴム片が多数確認されたことにより, ゴム片が皮下内に注入される可能性が強く示唆された. コアリングの原因としては, 針を同一個所に回転させて刺すためと考えられる. そのため, 今後はペン型注射器への針の装着について構造上の改良が必要である. コアリングは注射液の異物混入という点で, 医学的にも薬学的にも非常に重大な問題である. 今後はラテックスアレルギーやリポディストロフィーなどとの関連も検討する必要がある.

著者

西田 篤司

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.141, no.8, pp.985-994, 2021-08-01 (Released:2021-08-01)

参考文献数

32

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On the occasion of receiving the Pharmaceutical Society of Japan Award 2020, I explained our research activities on the total syntheses of polycyclic alkaloids as an invited review. The structure of lundurine B, which has an unstable cyclopropane fused indoline skeleton, was proved firstly by the total synthesis. I also describe the total syntheses of optically active lundurine B and rapidilectine B utilizing asymmetric desymmetrization of the spiro intermediate. We developed an intramolecular bond formation reaction between the 2-position of the furan ring to the iminium cation (furane-iminium cation cyclization) to synthesize manzamine alkaloids. The reaction was applied to the total synthesis of the core skeleton of nakadomarin A and ircinal A. A ring-closing metathesis reaction effectively applied to the synthesis of medium and large heterocyclic rings containing the cis double bond found in the structures of nakadomarin A and ircinal A. The total synthesis of schizocommunin, a metabolite of Schizophyllum commune isolated from a patient with human allergenic bronchopulmonary mycosis, was accomplished. We could correct the error in the proposed structure by total synthesis of the natural product. A part of the mechanism of cytotoxicity expression was clarified using newly synthesized shizocommunin.

著者

菊池 千草 堀 英生 前田 徹 松永 民秀 鈴木 匡

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.131, no.3, pp.477-483, 2011-03-01 (Released:2011-03-01)

参考文献数

10

被引用文献数

2 3

---

One of the Specific Behavioral Objectives (SBOs) of pharmaceutical education model-core curriculum is as follows: “Understand patient's state of mind and be sensitive to patient's feelings”. We performed learning through simulation of diabetes drug therapy as a means to achieve the objective and evaluated the educational effects of the learning. The simulation was performed and a questionnaire survey was conducted among the 4th-year students of the 6-year curriculum before and after simulation. The score of “level of understanding patient's feelings” was significantly increased after simulation (p<0.001). In addition, the score tended to be associated (R2=0.192) with an increased score in two factors that affect patients' self-care action: “Consciousness of diabetes mellitus” (β=0.251, p=0.062) and “Time and effort for drug therapy” (β=0.248, p=0.065). The main topics of discussion about the simulation included “Lack of sense of critical illness”, “Lifestyle”, “Dose regimen” and “Necessity of support from patients' family and others close to them”. Therefore, the learning through simulation diabetes drug therapy was effective to understand patients' states of mind because students learned the importance of some factors affecting self-care action.

著者

菊池 千草 松永 民秀 鈴木 匡

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.6, pp.809-820, 2015-06-01 (Released:2015-06-01)

参考文献数

13

被引用文献数

2 3

---

Pharmacy school students were trained in a program simulating medication administration and giving adherence instructions. Following the training, the educational effects were evaluated. Students were separated into two groups. One group of students played the role of pharmacists and instructed simulated patients on medication adherence. Another group of students played the role of patients receiving simulated drug therapy; they were instructed on medication adherence by the students playing the role of pharmacists. The educational effects were evaluated using a questionnaire. The scores for “recognition of factors that influence medication adherence” tended to increase after the simulation, and they increased significantly after practical training. The scores for “self-evaluation of technique for instructing patients on medication adherence” increased significantly after the simulation, and they increased even more after practical training. The students' understanding of the effects on patients who were being instructed also increased significantly after the simulation, and these changes were maintained after practical training. In particular, students became more aware of the influence of pharmacists' attitudes. In practical training, the simulation training was helpful for bedside practice at hospital pharmacies and over-the-counter service at community pharmacies. Thus, the use of role play and simulated patients was an effective method for training pharmacy students to instruct patients on medication adherence.

著者

笠井 博子 久保田 結

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.138, no.12, pp.1569-1577, 2018-12-01 (Released:2018-12-01)

参考文献数

16

被引用文献数

1

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Volatile components originating from Lavandula angustifolia Hidcote and Lavandula x intermedia Grosso plants cultivated in a medicinal plant garden of Hoshi University located in southern Tokyo were investigated using thermal desorption-GC-MS. Sampling of the flowers and herbs of the lavender was performed at different developmental stages, i.e., summer, autumn, and winter (herbs only) using solid phase micro extraction fibers. Linalool, linalyl acetate, β-caryophyllene, β-myrcene, α-ocimene, β-ocimene, and terpinen-4-ol were the predominant constituents originating from the flowers of both plants. Additional volatile compounds such as borneol, eucalyptol, and camphor were found in the Lavandula x intermedia flowers. The number of volatile compounds originating from the Lavandula angustifolia flowers in summer was greater than that in autumn. 3-Hexen-1-ol, 3-carene, and p-cymen-8-ol were volatile compounds characteristic of the herbs, and α-ocimene, allo-ocimene, and terpinen-4-ol were detected only from flowers. In comparing volatile compounds obtained from fresh herbs with those from dried herbs, camphor, β-caryophyllene, and borneol were absent in dried herbs. For people who visit the plant garden, smelling the fragrances of plants directly is believed to deliver not only pleasure but also beneficial therapeutic properties.

著者

前田 真之

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.141, no.8, pp.995-1000, 2021-08-01 (Released:2021-08-01)

参考文献数

22

被引用文献数

1

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Over the past few decades, the effectiveness of antibiotics has been diminished owing to the emergence of antimicrobial resistance resulting from the overuse of antibiotics. Antimicrobial stewardship aims to improve the appropriateness of antibiotic use to reduce antimicrobial resistance and benefit patients. Antimicrobial stewardship requires structural prerequisites for implementing antimicrobial stewardship programs (ASPs), such as the presence of a multidisciplinary antimicrobial stewardship team (AST), to ensure appropriate antimicrobial use at healthcare facilities. However, manpower shortage for ASTs in most Japanese hospitals has resulted in limited implementation of ASPs. Our study provided a directive for promotion of comprehensive ASPs including various outcome measures. Our findings would provide useful benchmarks for hospitals planning to implement ASPs in Japan as well as around the world. This review provides a framework for evaluating the outcome measures and benchmarks of ASPs based on our study.

著者

佐藤 浩輔

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.133, no.10, pp.1041-1053, 2013-10-01 (Released:2013-10-01)

参考文献数

46

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It is important that various lesions in DNA were detected selectively and conveniently to know mechanisms of carcinogenicity and/or aging of cells. However, most detection methods of DNA lesion are complicated and take a long time for enzymatic hydrolysis and analysis by HPLC and/or mass spectrometry. This review shows the new concept for detection of DNA lesion by “fluorogenic reagent”. Inspired by the unique bis-heteroaryl structure of luciferin and 5-heteroaryl-2′-deoxyuridine having good fluorescence properties, we designed and synthesized fluorogenic reagent 4,5-dimethoxy-2-aminothiophenol for a selective and convenient detection for 5-formyl-2′-deoxyuridine, which is generated in yields comparable to that of 2′-deoxy-8-oxoguanosine, in DNA. Generated 5-(5,6-dimethoxybenzothiazol-2-yl)-2′-deoxyuridine has a high quantum yield and larger Stokes shift in aqueous solution. This derivatization of 5-formyl-2′-deoxyuridine in oligodeoxynucleotide occurred quickly and quantitatively. The fluorogenic reagent was also revealed to detect 5-formyl-2′-deoxyuridine in γ-irradiated calf thymus DNA with irradiation dose dependent manner. Thus, our fluorogenic strategy enables to selective and convenient detection of lesion in DNA exposed to various forms of oxidative stress.

著者

新井 賢 藤本 憲二 橋本 竹二郎 滝島 常雄 小屋 佐久次

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.107, no.4, pp.279-286, 1987-04-25 (Released:2008-05-30)

参考文献数

13

被引用文献数

3 3

---

In order to identify the constituents of ethanol-extractable amino acids from Pinus densiflora SIEB. et ZUCC. leaves, high performance liquid chromatography (JASCO TWINCLE amino acids analyzer system) was used. According to the results obtained, ethanol-extractable amino acids confirmed to be such 19 different kinds, as Asp, Thr, Ser, Asn, Glu, Gln, Pro, Gly, Ala, Val, Met, Ile, Leu, Tyr, Phe, Lys, His, Arg and γ-aminobutyric acid (GABA). There was a seasonal fluctuation in the amount of free amino acids constituent, and three different patterns of changing in the amount were noticed. The major constituents of free amino acids were found to be GABA and Ala. There were similarities in the patterns of free amino acids contents among new buds, one year leaves and two year leaves. However few amount of Met and His were detected from the stage of the new buds than any other. Basic amino acids were found more in the one year leaves and the two year leaves than in the new buds. The contents of Gln, Lys and Arg increased in the germination stage of the new buds, and the contents of GABA, Pro, Ala and Asn decreased in the growing stage of the new shoots. The above facts lead to the conjecture of that these free amino acids were involved deeply in the growth of Pinus densiflora SIEB. et ZUCC. leaves.

著者

岡 夏未 近藤 真志 松原 秀樹 出石 啓治 田坂 祐一

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.141, no.7, pp.979-984, 2021-07-01 (Released:2021-07-01)

参考文献数

12

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Drug-drug interactions (DDIs) are responsible for an increase in the incidence of adverse drug reactions. Although CYP is known to be involved in metabolic processes, the DDIs among three or more drugs that involve the same CYP molecular species have not been fully investigated. In this study, we retrospectively examined the relationship between the number of drugs and potential DDIs in metabolic processes involving CYPs in patients who picked up their prescribed drugs at 11 pharmacies in the Kojima Branch of the Okayama Pharmaceutical Association. We found that 66.5% of the 924 patients had potential DDIs; more than half of the patients who took six or more drugs had potential DDIs among three or more drugs. The mean number of CYP3A4-related drugs involved in potential DDIs was 3.52±1.56 in patients who took seven drugs, suggesting the need for careful monitoring of specific symptoms and blood test results for the early detection of adverse drug reactions caused by DDIs among three or more drugs.

著者

上村 静香 西原 正和 大住 優子 塩田 裕徳

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.139, no.11, pp.1471-1478, 2019-11-01 (Released:2019-11-01)

参考文献数

25

被引用文献数

3

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Phellodendron bark (“Obaku”) is an important crude drug used in Kampo-medicine. Recently, powder formulation of phellodendron bark was approved as an “efficacious treatment for bruise, sprain, and periodontal diseases”, and it has been marketed as an OTC agent. To obtain this approval, the examination of quality control-related characteristics is necessary. Therefore, we established a quantitative method for jatrorrhizine, palmatine, and berberine determination. In this study, we compared the contents of the three constituents obtained from the extracts of Japanese and Chinese phellodendron bark and found remarkable difference.

著者

合田 幸広

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.141, no.6, pp.787-791, 2021-06-01 (Released:2021-06-01)

参考文献数

11

被引用文献数

3

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The author believes that the three pillars of pharmaceutical sciences (PS) in Japan are drug development science, medical pharmacy, and quality management science. Of these, the most PS-like science is quality management science, both historically and presently. Considering the balance of safety and efficacy is the basis of PS. The definition of “quality” is the degree to which a set of inherent properties of a product, system, or process fulfills requirements in Q9 of International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH). In our society, pharmaceutical science graduates including pharmacists, are active participants, not only in the pharmaceutical industry, including a pharmacy, but also in the food industry, especially for quality assurance and quality control. This report presents a focused overview of quality in health foods, foods with health claims, and pharmaceutical products and discusses the importance of a curriculum focusing on quality assurance, control, and management in pharmaceutical education.

著者

柳 奈津代 佐藤 宏樹 澤田 康文

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

pp.21-00001, (Released:2021-05-24)

参考文献数

11

被引用文献数

1

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Previous studies have reported the inappropriate administration of medication at nursery schools by the staff and a lack of drug-related information from caregivers at the time of request. However, the situation concerning medication administration at nursery schools from the mothers’ perspective is unknown and it is not clear what information the mothers provided to nursery staff at the request. We conducted an online survey between April and May 2019 regarding the administration of medication at the nursery school with input from 600 mothers. Overall, 510 (85%) individuals replied that the requests to administer medication were acceptable for all or some of the medications. Application forms for medications were used by 91% of the 301 mothers who had previously made such requests. Although information including the child’s name, medication times, illness of the child, parent’s name, and dosage form was specified by over 70% of mothers, drug-related information such as effectiveness, side effects, and drug interactions was insufficient. In total, 41 instances of inappropriate medication administration by staff were reported by 35 mothers. It is suggested that the drug information sheets provided by community pharmacies should make up for inadequate drug-related information on application forms for medications to avoid the risk of adverse events and reduce staff burden. Toward this end, it is necessary to provide easily understandable information sheets for nursery staff, as the medication is usually administered by nursery staff, not a nurse. Community pharmacists should support these measures as pharmaceutical professionals.

著者

添田 真司 高柳 理早 渡邊 昌之 山田 安彦

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.137, no.5, pp.589-593, 2017 (Released:2017-05-01)

参考文献数

13

被引用文献数

1

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In this study, we established a methodology to calculate the rate of overlooking a dispensing error (inspecting error rate) as a new index for the purpose of determining dispensing error and malpractice rates. Using data obtained from analyses of these error rates at our and two other hospitals, an inspecting error rate was calculated for each institution. Our results showed that inspecting errors occurred at a frequency 3-5 times greater as compared to dispensing errors at each of the examined hospitals. We concluded that construction of a higher quality safety management system would be enabled by incorporation of an inspecting error rate as a new index to evaluate medical safety in regard to dispensing of medicines and managing inspection accuracy.

著者

堤 康央

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.141, no.6, pp.813-816, 2021-06-01 (Released:2021-06-01)

参考文献数

6

---

For human health and welfare, toxicology/safety science is a branch of the pharmaceutical sciences dealing with the risk or benefit of pharmaceutical products derived from organic compounds, proteins, and genes, as well as chemicals contained in cosmetics or food additives. The quality of pharmaceutical products is one of the factors that decide risk or benefit, so quality assurance based on regulatory science is an important research and education area in the field of toxicology/safety science.

著者

国友 順一 山本 知恵子 大槻 多嘉子

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.11, pp.1141-1142, 1964-11-25 (Released:2010-02-19)

参考文献数

4

被引用文献数

3 9

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Alkaloids contained in the so-called primitive lotus were examined and components similar to domestic lotus (Nelumbo nucifera GAERTN.), roemerine (I), nuciferine (II), nornuciferine (III), and dl-armepavine (IV), were isolated in crystalline form and identified (cf. Table I).

著者

佐藤 悠介 畠山 浩人 兵藤 守 秋田 英万 原島 秀吉

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.12, pp.1355-1363, 2012-12-01 (Released:2012-12-01)

参考文献数

19

被引用文献数

5 7

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The development of a carrier for the delivery of siRNA is a factor in the realization of RNA interference (RNAi) therapeutics. Modification of siRNA carriers with polyethylene glycol, i.e., PEGylation, is a general strategy for stabilizing a particle in the blood stream and delivering it to tissue or cells. However, it is well-known that, when a carrier is modified by PEGylation, it results in a significant inhibition of both cellular uptake and the endosomal escape process. In a previous study, we reported on the development of a multifunctional envelope-type nano device (MEND) for delivering siRNA and peptide-based functional devices for overcoming the effects conferred by PEGylation and succeeded in the delivery of siRNA to tumor tissue. In this study, we noticed that the pH-sensitive property, changing from neutral to cationic in response to a decrease in pH, could avoid the inhibition caused by PEGylation and succeeded in synthesizing a pH-sensitive cationic lipid, YSK05. The YSK05-MEND had a higher fusogenicity and potency for endosomal escape than other MENDs containing conventional cationic lipids. The PEGylated YSK05-MEND induced efficient gene silencing and avoided the inhibition of endosomal escape caused by PEGylation followed by optimization of the lipid composition. Furthermore, the intratumoral injection of the PEGylated YSK05-MEND resulted in a more efficient gene silencing compared with MENDs containing conventional cationic lipids. Thus, the YSK05-MEND is a promising siRNA carrier for avoiding the inhibition in intracellular trafficking caused by PEGylation both in vitro and in vivo.

著者

山本 郁男

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.1, pp.73-120, 2005-01-01 (Released:2005-01-01)

参考文献数

91

被引用文献数

2 3

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Thirty-six allyl substituted oxopyrimidine analogues such as barbituric acid (BA), barbiturates, uracil, thymine, and related derivatives including 13 new compounds were synthesized and their pharmacologic effects ([hypnotic activity, anticonvulsant activity against pentylentetrazol (PTZ)-induced seizures, and LD50]) and interactions with the barbiturates were evaluated in mice and rats. The results are briefly and parially summarized as follows. BA prolonged pentobarbital (PB)-induced sleep and had some central depressant effects. N,5,5-Triallyl-BA exhibited some hypnotic and anticonvulsant activities, although the other 5,N-allyl-compounds did not show any activity except for allobarbital (AlloB). N-Allyl-BA, 5-allyl-BA, N1,N3,5-triallyl-BA, N,5,5-triallyl-BA, and N1,N3,5,5-tetraallyl-BA also prolonged PB-induced sleep. Interestingly, N,5,5-triallyl-BA was the most potent in the interaction with AlloB, phenobarbital (PheB), amobarbital (AB), PB, and thiopental (TP) but not barbital (B). N1,N3,5,5-Tetraallyl-BA prolonged AlloB-, PB-, and AB-induced sleep but not B-, PheB-, and TP-induced sleep. N1,N3,5-Triallyl-B prolonged only PB- and TP-induced sleep. 5,5-Diallyl-BA prolonged PheB- and TP-induced sleep. N,5-Diallyl-BA prolonged only TP-induced sleep. In contrast, BA and N1,N3,5-triallyl-AB tended to antagonize AlloB, AB, and B. N1,N3,5,5-Tetraallyl-BA also slightly antagonized B, PheB, and TP. 5,5-Diallyl-BA antagonized only AB. The prolonging effects of BA, N,5,5-triallyl-BA, and N1,N3,5,5-tetraallyl-BA on PB-induced sleep were dose dependent. These results indicate that the position and number of allyl groups substituted on the structure of BA play an important role in their depressant activities. This review deals with the structure-activity relationship of allyl-substituted oxopyrimidines as part of our search for antagonists and agonists of barbiturates as well as their mechanisms of action.