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flutazolam (Coreminal / flutazolam)

✓ Approved

Mitsubishi Tanabe Pharma Corporation · GABRA1 · 小分子

什么是 flutazolam?

flutazolam 是一种小分子,由Mitsubishi Tanabe Pharma Corporation研发。该药已获批,用于治疗相关适应症。

药物档案

商品名Coreminal, flutazolam
公司Mitsubishi Tanabe Pharma Corporation
药物类别小分子
分子靶点GABRA1, GABRA2, GABRA3, GABRA5
状态Approved

作用机制

分子靶点

flutazolam 作用于 4 个分子靶点:

GABRA1gamma-aminobutyric acid type A receptor alpha1 subunit (DEE19, ECA4)
GABRA2gamma-aminobutyric acid type A receptor alpha2 subunit (DEE78, EIEE78)
GABRA3gamma-aminobutyric acid type A receptor alpha3 subunit (EPILX2)
GABRA5gamma-aminobutyric acid type A receptor alpha5 subunit (EIEE79, DEE79)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

flutazolam 针对 1 个适应症,涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersAnxiety✓ Approved

相关研究文献

PubMedDrug testing and analysis2016-07-02

Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assays.

Pettersson Bergstrand Madeleine M, Helander Anders A, Hansson Therese T, Beck Olof O

The emerging new psychoactive substances made available for recreational drug use have recently started to include designer benzodiazepines. As a consequence, the routine immunoassay drug testing for benzodiazepines may become less effective, due to an increased occurrence of 'false negative' and 'false positive' results. This work aimed to extend the knowledge of analytical cross-reactivity of 13 designer benzodiazepines in the CEDIA, EMIT II Plus, HEIA, and KIMS II immunoassays. Urine standards were prepared by spiking blank urine with clonazolam, deschloroetizolam, diclazepam, estazolam, etizolam, flubromazepam, flubromazolam, flutazolam, 3-hydroxyphenazepam, meclonazepam, nifoxipam, phenazepam, and pyrazolam. Authentic urine samples from intoxication cases identified by liquid chromatography-tandem mass spectrometry (LC-MS/MS) were also investigated. For the spiked standard samples, the 13 designer benzodiazepines generally showed a high cross-reactivity in all assays. This was further confirmed when investigating their detectability in authentic urine samples from cases of drug intake. The test responses also indicated additional reactivity from metabolites. The lowest detectability in spiked samples was observed for flutazolam, which shows the most divergent chemical structure compared with the other benzodiazepines. Overall, the KIMS II and CEDIA immunoassays, which both include enzymatic hydrolysis of conjugated forms, showed the highest, and EMIT II Plus the lowest degree of reactivity, for spiked parent substances and authentic urine specimens. The results of this study demonstrated that designer benzodiazepines can be detected in standard urine immunoassay drug screening and this should be taken into consideration when performing confirmation analysis. Copyright © 2016 John Wiley & Sons, Ltd.

PMID 27366870
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PubMed[Hokkaido igaku zasshi] The Hokkaido journal of medical science1988-03-01

[Studies on the clinical significance concerning the changes in serum pepsinogen-I and gastrin levels in aged patients with chronic gastritis].

Hamada Y Y, Kamiya K K, Koyama M M, Asaka M M et al.

Of 86 cases of aged patients with chronic gastritis treated with Trimebutine or Flutazolam, we evaluated the changes of serum pepsinogen-I and gastrin levels in their clinical courses from the points of the correlation with severity of chronic gastritis, aging phenomenon and the changes of symptom and endoscopic findings. In order to elucidate the multidimensional interrelation among these items, we used Hayashi's quantification theory II as a conventional analysis method. In aged patients, generally, although the serum gastrin levels were rather high compared with younger generation, the serum pepsinogen-I levels were consistently low throughout their clinical courses. There were some correlation between the levels of serum gastrin and the severity of chronic gastritis. When the drugs were effective on improving the condition of the disease, the level of gastrin revealed gradual decrease. These changes of gastrin were more typical in patients treated with Trimebutine.

PMID 2898425
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PubMedYakugaku zasshi : Journal of the Pharmaceutical Society of Japan1987-10-01

[The behavior of 1,4-benzodiazepine drugs in acidic media. IX. Effect of hydrolyzate of flutazolam on the central nervous system].

Yashiro T T, Kuwayama T T, Kawazura H H, Suzuki T T

PMID 2894449
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PubMedChemical & pharmaceutical bulletin1986-01-01

The behavior of 1,4-benzodiazepine drugs in acidic media. V. Kinetics of hydrolysis of flutazolam and haloxazolam in aqueous solution.

Kuwayama T T, Kurono Y Y, Muramatsu T T, Yashiro T T et al.

PMID 2870816
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PubMedNihon yakurigaku zasshi. Folia pharmacologica Japonica1978-11-01

[Psychopharmacological effects of flutazolam (MS-4101) (author's transl)].

Mitsushima T T, Ueki S S

Behavioral effects of Flutazolam (MS-4101), a new derivative of benzodiazepines, was investigated and compared with effects of diazepam in mice and rats. MS-4101 suppressed hyperemotionality in septal rats, fighting behavior in long-term isolated mice and pentylenetetrazol convulsion and potentiated thiopental sleep. These effects of MS-4101 were the same in potency as those of diazepam. MS-4101 was more potent than diazepam in reducing the spontaneous locomotor activity in the open-field test and potentiating the stimulant effect of methamphetamine on locomotor activity. On the other hand, suppression of hyperemotionality in O. B. rats, potentiation of ethanol-induced anesthesia, prevention of maximal electroshock, prevention of strychnine convulsin and muscle relaxant effect of MS-4101 were less potent than in the case of diazepam. MS-4101 had also an anticonflict effect, which was less potent than that seen with diazepam. Suppression of locomotor activity was potentiated by chronic administration of MS-4101, but disappeared with chronic administration of diazepam. MS-4101 inhibited considerably both scratching and head-twitch induced by mescaline in mice. Scratching was increased with small doses of diazepam and decreased with high doses. Head-twitch was decreased with small doses of diazepam and increased with high doses.

PMID 750333
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