Über Synthesen spasmolytisch wirkender Stoffe. II. Mitteilung

Külz, Fritz; Rosenmund, Karl W.; Kayser, Erich; Schwarzhaupt, Otto; Sommer, Heinz

doi:10.1002/cber.19390721224

Cited by 7 publications

(3 citation statements)

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“…Alverine was first described in 1939 as having been synthesized as a synthetic analog of papaverine, a smooth muscle relaxant. 18,19 It has been used since then as an antispasmodic in the treatment of irritable bowel syndrome, a poorly defined condition that can present with diarrhea or constipation. 17 Therapeutic benefit in irritable bowel syndrome has been variable.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

“…Alverine was first described in 1939 as having been synthesized as a synthetic analog of papaverine, a smooth muscle relaxant. , It has been used since then as an antispasmodic in the treatment of irritable bowel syndrome, a poorly defined condition that can present with diarrhea or constipation . Therapeutic benefit in irritable bowel syndrome has been variable. , Alverine has not been well studied for its mechanism of action, although it has been described as an antagonist of the 5-hydroxytryptamine 1A (5-HT 1A ) receptor …”

Section: Results and Discussionmentioning

confidence: 99%

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Identification of Alverine and Benfluorex as HNF4α Activators

et al. 2013

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The principal finding of this study is that two drugs, alverine and benfluorex, used in vastly different clinical settings and previously unknown to share mechanistic or structural similarity, activated the nuclear receptor transcription factor HNF4α. Both were hits in a high-throughput screen for compounds that reversed the inhibitory effect of the fatty acid palmitate on human insulin promoter activity. Alverine is used in the treatment of irritable bowel syndrome, while benfluorex (Mediator) was used to treat hyperlipidemia and type II diabetes. Benfluorex was withdrawn from the market recently because of serious cardiovascular side effects related to fenfluramine-like activity. Strikingly, alverine and benfluorex have a previously unrecognized structural similarity, consistent with a common mechanism of action. Gene expression and biochemical studies revealed that they both activate HNF4α. This novel mechanism of action should lead to a reinterpretation of previous studies with these drugs and suggests a path towards the development of therapies for diseases such as inflammatory bowel and diabetes that may respond to HNF4α activators.

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Section: ■ Results and Discussionmentioning

confidence: 99%

Section: Results and Discussionmentioning

confidence: 99%

Identification of Alverine and Benfluorex as HNF4α Activators

et al. 2013

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“…Amines b, c, and eem were purchased from several providers. N-Ethyl-3-phenylpropan-1-amine (d) was synthesized according to known procedures [55]. Vesamicol hydrochloride was purchased by BIOTREND Chemikalien GmbH, Germany and cyclohexene oxide by SigmaeAldrich, Germany.…”

Section: Instruments and Materialsmentioning

confidence: 99%