Benzodiazepines and Anxiolytics

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L1764 (±)-Lorazepam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
    • C5174 4′-Chlorodiazepam ≥98% (TLC) 4′-Chlorodiazepam (Ro5-4864) is a potent selective antagonist of the mitochondrial translocator protein 18kDa (TSPO), formerly known as the peripheral benzodiazepine receptor (PBR). Ro5-4864 does not bind to GABA(A) receptors and lacks typical benzodiazepine effects, but has been found to be neuroprotective in several studies.
    • A1862 Alpidem ≥98% (HPLC), powder Alpidem is a potent antagonist of peripheral benzodiazepine receptor (PBR) that is located on the outer mitochondrial membrane and interacts with the mitochondrial permeability transition (MPT) pore. Alpidem is an anxiolytic drug from the imidazopyridine family. Alpidem acts selectively on the α3 receptor subtype and to a lesser extent at the α1 subtype (Kd of 0.33nM and 1.67nM respectively), of the benzodiazepine receptor.
    • A8800 Alprazolam Alprazolam binds the GABAA receptor at the benzodiazepine site, which is different than the ligand-binding site at which GABA binds. Alprazolam has been shown to be an anxiolytic (anti-anxiety agent) as well as having anticonvulsant, muscle relaxant and antidepressant activity.1
    • B4938   Benzodiazepine Receptor, Peripheral human membrane suspension Membranes are suspended in 50 mM Tris-HCl containing 10% sucrose, (pH 7.4 at 25 °C).
    • B6434 Bretazenil >98% (HPLC), solid Bretazenil is a benzodiazepine partial agonist.
    • C6862 CB 34 >98% (HPLC) Selective high affinity ligand at peripheral benzo­diazepine receptors.
    • C4024 Carbamazepine powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Sodium channel inhibitor.
    • C8414 Clobazam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
    • C1277 Clonazepam powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site.
    • D7282 Desmethyldiazepam analytical standard, for drug analysis Primary metabolite of diazepam; ligand for the GABAA receptor benzodiazepine modulatory site.
    • D0899 Diazepam Benzodiazepine anxiolytic; prototype ligand for the GABAA receptor benzodiazepine modulatory site.
    • E3638 Estazolam Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site.
    • SML0272 Etifoxine hydrochloride ≥98% (HPLC) Etifoxine is an anxiolytic anticonvulsant, which promotes axonal regeneration. It binds to β2 and β3 subunits of the GABAA receptor complex, a different target site to benzodiazepines, and binds to the translocator protein (18 kDa) TSPO, formerly known as the peripheral or mitochondrial benzodiazepine receptor. TSPO carries cholesterol from the outer to the inner mitochondrial membrane, which is the rate-limiting step of steroidogenesis. Whereas, its anxiolytic effects involve GABAA receptors and TSPO, etifoxine′s neuroregenerative effects mainly involve TSPO.
    • F6300 Flumazenil >99% (HPLC), solid Highly specific benzodiazepine receptor antagonist.
    • F9261 Flunitrazepam Hypnotic; anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
    • F103 Flurazepam dihydrochloride solid Benzodiazepine anxiolytic; anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site.
    • SML0645   Iomazenil ≥98% (HPLC) New Iomazenil (Ro 16–0154) is a benzodiazepine competitive antagonist and partial inverse agonist. Iomazenil has been shown to counteract the effects of alcohol.
    • L9787 L-655,708 ≥98% (HPLC), powder Novel ligand selective for the benzodiazepine site of GABAA receptors which contain the α5 subunit.
    • M2419 Midazolam maleate salt Sedative/Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site; CYP3A4 substrate.
    • D8555 N,N-Dihexyl-2-(4-fluorophenyl)indole-3-acetamide High affinity ligand for glial mitochondrial benzodiazepine receptors; stimulates neurosteroid biosynthesis; does not bind GABAA receptors
    • N3889 Nitrazepam Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site.
    • N2144 Norfludiazepam analytical standard, for drug analysis The major human metabolite of flurazepam
    • O5254 Oxazepam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
    • C0424 PK 11195 Peripheral benzodiazepine antagonist.
    • P3654 Prazepam Anxiolytic
    • R109 Ro 15-4513 solid Benzodiazepine receptor partial inverse agonist; anxiogenic; ethanol antagonist.
    • T9772 Triazolam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
    • Z103 Zolpidem ≥98% (HPLC), solid Potent and selective agonist for the benzodiazepine receptor associated with the GABAA receptor; hypnotic.
    • Z4900 Zopiclone Benzodiazepine receptor agonist
    • H9149 α-Hydroxyalprazolam powder, ≥98% (TLC) Alprazolam metabolite
    • H2529 α-Hydroxytriazolam Triazolam metabolite
    • E006 β-Carboline-3-carboxylic acid N-methylamide Benzodiazepine inverse receptor agonist; potent anxiogenic agent.
    • SML0249 βCCt ≥98% (HPLC) βCCt has been characterized as an α1selective antagonist and benzodiazepine mixed agonist/antagonist.. A recent study found Ki values for the GABA-A subtypes were 0.72, 15, 18.9, 110.8, and >5,000 nM at five recombinant GABAA/BzR subtypes α1, α2, α3, α5, and α6 respectively. βCCt was a near ‘neutral’ antagonist (i.e., little or no efficacy) at all these 5 recombnant GABAA/BzR receptor subtypes. βCCt has been shown to reduce alcohol self-administration in alcohol preferring (P) and high alcohol drinking (HAD) rats.