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Diazepam alkyne
Product key features
- Bioorthogonal Reactivity: Contains a terminal alkyne group compatible with copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) for selective conjugation to azide-functionalized molecules.
- Pharmacophore Retention: Maintains the benzodiazepine core structure and activity, enabling studies on GABAA receptor interactions & related pharmacology.
- Versatile Probe Development: Ideal for synthesizing fluorescent, affinity, or photoactivatable probes for use in chemical biology & neuropharmacology.
- Live-Cell Compatibility: Suitable for intracellular labeling and target engagement studies in live-cell or in vivo systems.
- Research Applications: Facilitates structure–activity relationship (SAR) studies, target identification, and imaging of benzodiazepine derivatives in complex biological environments.
Product description
Diazepam alkyne is an alkyne-functionalized derivative of diazepam designed for bioorthogonal conjugation via copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC), commonly referred to as “click chemistry.” Incorporation of a terminal alkyne group enables site-specific and chemoselective coupling to azide-bearing molecules, including fluorophores, biotin derivatives, and solid-phase supports. The compound preserves the core benzodiazepine scaffold and pharmacophore of diazepam, facilitating its use in neuropharmacological research applications such as GABAA receptor binding assays, photoaffinity labeling, and probe development. Diazepam alkyne is particularly useful for generating functionalized analogs suitable for imaging, pull-down experiments, and structure–activity relationship (SAR) studies. Its compatibility with live-cell labeling strategies allows researchers to investigate the distribution, uptake, and target engagement of diazepam-like compounds in physiologically relevant systems. This reagent provides a powerful platform for elucidating benzodiazepine mechanisms of action at the molecular level.
References
View all 6 references: Citation Explorer
Synthesis, Molecular Docking and In Vivo Biological Evaluation of Iminostilbene Linked 1,2,3-Triazole Pharmacophores as Promising Anti- Anxiety and Anti-Inflammatory Agents.
Authors: Ankali, Kariyappa N and Rangaswamy, Javarappa and Shalavadi, Mallappa and Naik, Nagaraja
Journal: Medicinal chemistry (Shariqah (United Arab Emirates)) (2022): 260-272
Authors: Ankali, Kariyappa N and Rangaswamy, Javarappa and Shalavadi, Mallappa and Naik, Nagaraja
Journal: Medicinal chemistry (Shariqah (United Arab Emirates)) (2022): 260-272
GABAergic mechanisms involved in the prepulse inhibition of auditory evoked cortical responses in humans.
Authors: Inui, Koji and Takeuchi, Nobuyuki and Sugiyama, Shunsuke and Motomura, Eishi and Nishihara, Makoto
Journal: PloS one (2018): e0190481
Authors: Inui, Koji and Takeuchi, Nobuyuki and Sugiyama, Shunsuke and Motomura, Eishi and Nishihara, Makoto
Journal: PloS one (2018): e0190481
Facile synthesis of new imidazo[1,2-a]pyridines carrying 1,2,3-triazoles via click chemistry and their antiepileptic studies.
Authors: Ulloora, Shrikanth and Shabaraya, Ramakrishna and Adhikari, Airody Vasudeva
Journal: Bioorganic & medicinal chemistry letters (2013): 3368-72
Authors: Ulloora, Shrikanth and Shabaraya, Ramakrishna and Adhikari, Airody Vasudeva
Journal: Bioorganic & medicinal chemistry letters (2013): 3368-72
The effects of diazepam on sensory gating in healthy volunteers.
Authors: van Luijtelaar, Gilles
Journal: Neuroscience letters (2003): 65-8
Authors: van Luijtelaar, Gilles
Journal: Neuroscience letters (2003): 65-8
Effects of (-)-baclofen, clonazepam, and diazepam on tone exposure-induced hyperexcitability of the inferior colliculus in the rat: possible therapeutic implications for pharmacological management of tinnitus and hyperacusis.
Authors: Szczepaniak, W S and Møller, A R
Journal: Hearing research (1996): 46-53
Authors: Szczepaniak, W S and Møller, A R
Journal: Hearing research (1996): 46-53
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