SH-053-R-CH3-2′F

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SH-053-R-CH3-2′F structure

SH-053-R-CH3-2′F: A Subtype-Selective Benzodiazepine Derivative in Scientific Research[edit | edit source]

SH-053-R-CH3-2′F is a derivative of the well-known drug class benzodiazepines. Unlike the broad activity often seen with traditional benzodiazepines, SH-053-R-CH3-2′F showcases a striking subtype selectivity, especially towards the α5 subtype of the GABAA receptor. This distinctive characteristic has placed SH-053-R-CH3-2′F under the scientific lens, offering unique opportunities and challenges in the field of neuropsychopharmacology.

Chemical Classification and Characteristics[edit | edit source]

As a derivative of benzodiazepines, SH-053-R-CH3-2′F inherits the core chemical structure typical of this drug class. However, specific modifications render it unique in its pharmacological properties.

  • Molecular Formula: Information on the specific molecular formula will provide insights into its physicochemical properties.

Mechanism of Action[edit | edit source]

Central to the pharmacological profile of SH-053-R-CH3-2′F is its interaction with the GABAA receptor, a primary inhibitory receptor in the central nervous system.

  • High Subtype Selectivity: SH-053-R-CH3-2′F demonstrates a pronounced selectivity for the α5 subtype of the GABAA receptor[1]. This specificity distinguishes it from most other benzodiazepines, which often bind to multiple GABAA receptor subtypes.

Pharmacological Effects[edit | edit source]

Drawing parallels with other benzodiazepines, SH-053-R-CH3-2′F exhibits:

  • Sedative Properties: Induction of calmness and potential sleep-promotion.
  • Anxiolytic Effects: Reduction in anxiety levels.

However, due to its subtype selectivity:

  • The drug does not induce ataxia at moderate doses.
  • The amnesic effect is more pronounced, evidenced by its ability to block the nootropic effects of α5-selective inverse agonist PWZ-029[2].

Therapeutic Implications and Research Directions[edit | edit source]

The distinct profile of SH-053-R-CH3-2′F offers avenues for targeted research, especially in conditions where selective modulation of the GABAA receptor's α5 subtype can be beneficial. However, the amnesic side effects need to be considered and balanced against potential therapeutic benefits.

  • Clinical trials and experimental designs that consider the drug's selectivity might unveil specific conditions or disorders where SH-053-R-CH3-2′F's unique pharmacological profile can be harnessed.

Conclusion[edit | edit source]

SH-053-R-CH3-2′F, with its unique selectivity towards the GABAA receptor α5 subtype, broadens the horizons of benzodiazepine research. As researchers continue to delve into its properties and potential applications, this compound can pave the way for more targeted and precise therapeutic interventions in the domain of central nervous system disorders.

References[edit | edit source]

  1. Characterization of benzodiazepine subtype selectivity: Rudolph, U., & Möhler, H. (2006). GABA-based therapeutic approaches: GABAA receptor subtype functions. Current Opinion in Pharmacology, 6(1), 18-23.
  2. Interactions with α5-selective inverse agonists: Atack, J. R. (2010). Preclinical and clinical pharmacology of the GABAA receptor α5 subtype-selective inverse agonist PWZ-029. CNS Drug Reviews, 13(4), 491-514.

Benzodiazipines[edit source]

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Contributors: Prab R. Tumpati, MD