LN733 Alprazolam: A Classic Triazolobenzodiazepine Reference Standard for Pharmacological and Forensic Research

Product Name: Alprazolam (LN733)
Chemical Name: 8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Common Designation: LN733
CAS Number: 28981-97-7
Molecular Formula: C₁₇H₁₃ClN₄
Molar Mass: 308.76 g/mol
Appearance: Fine, white crystalline powder

Introduction: The Benchmark Triazolobenzodiazepine

Alprazolam, cataloged under the research designation LN733, is arguably the most well-characterized and historically significant compound within the triazolobenzodiazepine class. Unlike novel analogs, Alprazolam boasts an extensive body of published scientific literature, making it an indispensable reference standard and a fundamental tool for comparative pharmacological research. Its structure—featuring a classic benzodiazepine core fused with a triazole ring and a chloro-substitution—serves as the prototypical model for understanding the triazolo subclass’s effects on pharmacokinetics and receptor interaction dynamics.

This product is provided as a high-purity chemical exclusively for non-human, in vitro research applications in qualified laboratory settings.

Key Characteristics and Research Properties

• Well-Established Pharmacological Profile: As a widely prescribed pharmaceutical, Alprazolam’s mechanisms of action, metabolic pathways, and receptor binding affinities are thoroughly documented. This makes it an ideal and reliable control compound for calibrating assays and validating experimental models against known data.

• Triazolo Ring Enhancement: The fusion of the triazole ring to the diazepine structure significantly increases its binding affinity for the benzodiazepine site on GABA-A receptors compared to earlier 1,4-benzodiazepines. It also contributes to a shorter elimination half-life, a key point of study in metabolic research.

• High Receptor Binding Affinity: Alprazolam is known for its high potency and selectivity as a positive allosteric modulator of the GABA-A receptor. Its well-defined inhibitory concentration (IC50) and binding affinity (Ki) values provide a crucial baseline for SAR studies comparing newer synthetic analogs.

• Defined Metabolic Pathway: Its primary metabolic pathway in humans, via hydroxylation by cytochrome P450 3A4 (CYP3A4) to alpha-hydroxyalprazolam, is well established. This makes it a perfect substrate for in vitro studies on CYP enzyme activity, drug-drug interactions, and metabolic stability assays.

Intended Applications and Research Use

Alprazolam (LN733) is a chemical for controlled scientific investigation and is not for human or veterinary use. It is a DEA Schedule IV controlled substance in the United States, and its handling is strictly regulated.

Its primary applications include, but are not limited to:

• Reference Standard in Forensic Toxicology: Serves as the primary calibrant and quality control standard for the development, validation, and routine use of analytical methods (GC-MS, LC-MS/MS, HPLC-UV) for the detection and quantification of benzodiazepines in biological samples.

• Pharmacological Control Studies: Used as a baseline comparator in in vitro receptor binding assays and functional activity studies to evaluate the relative potency and efficacy of novel or less-characterized GABA-A receptor modulators.

• Metabolic and Enzymatic Research: Investigation of cytochrome P450 3A4 (CYP3A4) enzyme kinetics, inhibition, and induction studies due to its well-documented role as a substrate for this key metabolic enzyme.

• Quality Assurance and Method Development: Essential for ensuring the accuracy and precision of analytical equipment and methodologies in research and forensic laboratories.

• Educational Tool: Used in academic settings to teach advanced techniques in analytical chemistry, pharmacology, and toxicology.

Handling, Storage, and Safety Information

• Purity: >99% (as verified by High-Performance Liquid Chromatography (HPLC) and Mass Spectrometry (MS)).

• Solubility: Soluble in organic solvents such as methanol, ethanol, chloroform, and dimethyl sulfoxide (DMSO). Slightly soluble in water.

• Storage: Must be stored in a tightly sealed container in a cool, dry, and dark environment to protect it from light and moisture. Long-term stability is best achieved when stored between +2°C and +8°C.

• Handling: CAUTION – CONTROLLED SUBSTANCE. This material is a potent compound and a regulated controlled substance. Researchers must hold the appropriate DEA registration and institutional approvals for its purchase, storage, and use. It must be handled in compliance with all federal and state regulations. Standard laboratory safety protocols must be followed, including the use of personal protective equipment (PPE) such as gloves and a lab coat. A fume hood is recommended for handling powders.