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概览

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

5-HT3 receptor(5-羟色胺受体3)	1

关联

1

项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的药物

Indisetron Hydrochloride

盐酸吲地司琼

靶点

5-HT3 receptor

作用机制

5-HT3 receptor拮抗剂

在研机构

北京嘉林药业股份有限公司 [+2]

原研机构

Nisshin Flour Milling Co Ltd

在研适应症

恶心和呕吐 [+2]

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

日本

首次获批日期2004-01-29

100 项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的临床结果

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0 项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的专利（医药）

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11

项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的文献（医药）

2006-11-01·YAKUGAKU ZASSHI4区 · 医学

ステロールを用いる生物活性化合物の合成と構造活性相関

4区 · 医学

Review

作者: TACHIBANA, Yoji

Sterols are widely and abundantly distributed in nature. It is convenient to utilize them for the preparation of useful compounds such as pharmaceuticals with steroid and secosteroid skeletons. This paper describes the synthesis and structure-activity relationships of naturally occurring active forms of vitamin D analogues, sterols having neurite outgrowth activity, and liver X receptor agonist. The active form of vitamin D(4) showed similar biological activities but had higher affinity to the vitamin D-binding protein compared with the corresponding vitamins D(2) and D(3). This shows that the active form of vitamin D(4) is a good candidate for an agent to replace the active forms of vitamins D(2) and D(3). In the course of screening for low molecular-weight compounds that exhibit neurite outgrowth activity in the culture broth, we found that the natural product dictyosterol showed strong activity. From screening of the analogues, it was found that the double bond between C22 and C23 in the side chain of the sterol is essential for its activity. Ergost-22-ene-1alpha,3beta-diol was found to serve as a stronger liver X receptor agonist than 24(S), 25-epoxycholesterol, which regulates the expression of genes involved in lipid metabolism. Structure-function study showed that the 1alpha-hydroxyl group, the saturated steroid structure, and the double bond between C22 and C23 are needed to function as a liver X receptor agonist.

2006-01-01·Journal of Nutritional Science and Vitaminology4区 · 医学

Comparative Oral Toxicity of Coenzyme Q10 and Its (2Z)-Isomer in Rats: Single and Four-Week Repeated Dose Toxicity Studies

4区 · 医学

Article

作者: Ikuo Yoshimura ; Shigeo Kawase ; Shigeki Hatakeyama

It has been reported that coenzyme Q10 (CoQ10) functions as an electron transfer carrier in mitochondria, and can produce an improvement in heart diseases such as congestive heart failure. Its (2Z)-isomer contains a cis-double bond at the 2-position of the decaprenyl side chain. As the original organic industrial synthesis of CoQ10 resulted in a product that contained a small amount of this isomer, the efficacy and safety of CoQ10 was determined using CoQ10 containing this isomer; however, no toxicity data have been reported for the (2Z)-isomer itself. Thus, we conducted single (2,000 mg/kg) and 4-wk repeated (1,000 mg/kg) oral dose toxicity studies in rats to compare the toxicological profiles of CoQ10 and its (2Z)-isomer. The two compounds displayed similar toxicological profiles, and it was concluded that neither CoQ10 nor its (2Z)-isomer produce toxic effects in rats in single or repeated doses.

Japanese Pharmacology & Therapeutics

The inhibitory action of indisetron hydrochloride, a 5-HT receptor antagonist, against the anticancer drug-induced emesis in the dog, ferret and suncus

作者: Tsuchiyama, Michio ; Minami, Masaru ; Taniguchi, Sugure ; Hamada, Tamiko ; Toru, Endo ; Hagihara, Koichiro

The inhibitory action of novel 5-HT₃ receptor antagonist indisetron hydrochloride (indisetron) against the anticancer drug-induced emesis was examined in the various animals.Cisplatin, the anticancer drug, induced acute emesis in the dog (the dose of cisplatin was 3mg/kg), ferret (10mg/kg) and suncus (50mg/kg).Cisplatin at the low dose (5mg/kg) induced acute (0-24 h) and delayed (24-72 h) emesis in the ferret.The other anticancer drug, cyclophosphamide (200mg/kg) also induced acute emesis in the ferret.The inhibitory action of indisetron was examined in all these emesis models and compared with granisetron or ondansetron in some models.Indisetron (1 mg/kg p.o.) inhibited the cisplatin-induced acute emesis in the dog, ferret and suncus.Granisetron inhibited the emesis in the dog with 0.3 mg/ kg p.o. but in the suncus with 10mg/kg p.o.Indisetron (1 mg/kg s.c. twice per day) also suppressed the low dose cisplatin-induced emesis in the ferret for acute and delayed phase.Ondansetron (1 mg/kg s.c. twice per day) did not suppress the cisplatin-induced emesis in the ferret for delayed phase but for acute phase.Indisetron (1 mg/kg p.o.) inhibited the cyclophosphamide-induced emesis in the ferret.From these results, we found that indisetron ameliorate the anticancer drug-induced emesis at several animals in the same dosage.Indisetron may be a useful drug that prevent the anticancer drug-induced emesis in the chemotherapy.

100 项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的药物交易

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100 项与 Nisshin Kyorin Pharmaceutical Co. Ltd. 相关的转化医学

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