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Thienotriazolodiazepine information


Core structure of thienotriazolodiazepines

A thienotriazolodiazepine[1] is a heterocyclic compound containing a diazepine ring fused to thiophene and triazole rings. Thienotriazolodiazepine forms the central core of several pharmaceutical drugs including:

  • α-Hydroxyetizolam
  • Brotizolam
  • Ciclotizolam
  • Clotizolam
  • Deschloroclotizolam
  • Deschloroetizolam
  • Etizolam
  • Flubrotizolam
  • Fluclotizolam
  • Fluetizolam
  • Metizolam

Thienotriazolodiazepines interact with the benzodiazepine receptor site, they typically have similar effects as 1,4-benzodiazepines (such as diazepam) and triazolobenzodiazepines (such as alprazolam).

Thienotriazolodiazepines that are not GABAA receptor positive allosteric modulators include:

  • Apafant
  • Israpafant[2]
  • JQ1
  1. ^ Catabay, A.; Taniguchi, M.; Jinno, K.; Pesek, J. J.; Williamsen, E. (1 March 1998). "Separation of 1,4-Benzodiazepines and Analogues Using Cholesteryl-10-Undecenoate Bonded Phase in Microcolumn Liquid Chromatography". Journal of Chromatographic Science. 36 (3): 113. doi:10.1093/chromsci/36.3.111.
  2. ^ Hirota, N; Yasuda, D; Hashidate, T; Yamamoto, T; Yamaguchi, S; Nagamune, T; Nagase, T; Shimizu, T; Nakamura, M (Feb 2010). "Amino acid residues critical for endoplasmic reticulum export and trafficking of platelet-activating factor receptor". Journal of Biological Chemistry. 285 (8): 5931–40. doi:10.1074/jbc.M109.066282. PMC 2820818. PMID 20007715.

and 18 Related for: Thienotriazolodiazepine information

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Thienotriazolodiazepine

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A thienotriazolodiazepine is a heterocyclic compound containing a diazepine ring fused to thiophene and triazole rings. Thienotriazolodiazepine forms...

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Deschloroetizolam

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Deschloroetizolam (also known as Etizolam-2) is a thienotriazolodiazepine that is the dechlorinated analog of the closely related etizolam. The compound...

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Fluetizolam

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2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects, which has...

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Fluclotizolam

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Fluclotizolam is a thienotriazolodiazepine derivative which was first synthesised in 1979, but was never marketed. It has subsequently been sold as a...

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Flubrotizolam

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2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects, which has...

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Metizolam

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Metizolam (also known as desmethyletizolam) is a thienotriazolodiazepine that is the demethylated analogue of the closely related etizolam. Following...

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Etizolam

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thiophene ring and triazole ring has been fused, making the drug a thienotriazolodiazepine. Although a thienodiazepine, etizolam is clinically regarded as...

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Thienodiazepine

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and R2 are part of a triazole ring, the substance is called a "thienotriazolodiazepine." The thienodiazepine structure forms the central core of some...

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Clotizolam

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Clotizolam (Ro11-1465) is a thienotriazolodiazepine derivative first invented in the 1970s, which in more recent years has been sold as a designer drug...

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Deschloroclotizolam

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Deschloroclotizolam is a thienotriazolodiazepine derivative which has been sold as a designer drug, first being identified in Sweden in 2021. Alprazolam...

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Brotizolam

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Brotizolam (marketed under brand name Lendormin) is a sedative-hypnotic thienotriazolodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic...

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Apafant

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factor (PAF). It was developed by structural modification of the thienotriazolodiazepine sedative drug brotizolam and demonstrated that PAF inhibitory actions...

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JQ1

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JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific...

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Ciclotizolam

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Ciclotizolam (WE-973) is a drug which is a thienotriazolodiazepine derivative. It is a partial agonist for the benzodiazepine site of the GABAA receptor...

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List of benzodiazepines

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very similar effects as benzodiazepines. Technically this is a thienotriazolodiazepine, but produces very similar effects as benzodiazepines. Flumazenil...

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Thienobenzodiazepine

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Thienobenzodiazepine is a heterocyclic compound containing a diazepine ring fused to a thiophene ring and a benzene ring. Thienobenzodiazepine forms the...

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Orally disintegrating tablet

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insomnia adults Etizest MD Consern etizolam Benzodiazepine analog/thienotriazolodiazepine Short-term treatment of anxiety and insomnia FazaClo AzurPharma...

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Israpafant

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developed for the treatment of asthma. Its chemical structure is a thienotriazolodiazepine, closely related to the sedative benzodiazepine derivative etizolam...

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