Adrenergic Receptors

Adrenergic receptor agonists and antagonists act on the receptors activated by norepinephrine and epinephrine. These receptors are G protein-coupled receptors (GPCRs), grouped into α1, α2 and β subtypes that control vascular tone, heart rate and metabolism. Cloning of the β-adrenergic receptor gene in 1986 revealed homology with rhodopsin, linking hormone receptors to the visual pigment family. In 2011 the crystal structure of the β2 adrenergic receptor bound to its G protein, Gs, captured an active receptor complex. Representative ligands include the α1 agonist phenylephrine HCl and the α1 antagonist prazosin HCl. The β agonist isoprenaline HCl and the β3-selective agonist mirabegron are also listed.

8 Items

  • Tandospirone citrate
    Cat. No.
    A18249

    Tandospirone citrate

    Synonyms: SM-3997 citrate

    Tandospirone citrate is a selective partial agonist of the 5-HT1A receptor, exhibiting a binding affinity with a Ki value of 27 nM. It demonstrates significant selectivity over other serotonin and adrenergic receptors, including SR-2, SR-1C, α1, α2, D1, and D2, with Ki values ranging from 1300 to 41000 nM. This compound is primarily used in research related to psychiatric disorders and anxiety management, making it a valuable tool for exploring serotonergic pathways and their implications in mental health.

    2 mg
    $25.00
    5 mg
    $40.00
    All 6 sizes
  • LY 178210
    Cat. No.
    A29759

    LY 178210

    LY 178210 is a selective partial agonist of the 5-HT1A receptor, exhibiting Ki values of 0.67 nM for 5-HT1A and 380 nM for 5-HT1D receptors, thereby demonstrating its specificity. Its minimal activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors makes it a valuable tool in neuropharmacology. Additionally, LY 178210 effectively inhibits forskolin-stimulated cyclase activity, though with lower potency compared to full agonists like 8-OH-DPAT. This compound is significant for studies on serotonergic modulation, as it markedly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the hypothalamus while increasing serum corticosterone concentrations.

    25 mg
    $2,285.00
    50 mg
    $2,935.00
    All 3 sizes
  • p-Iodoclonidine hydrochloride
    Cat. No.
    A57993

    p-Iodoclonidine hydrochloride

    p-Iodoclonidine hydrochloride is a partial agonist of the α2-adrenergic receptor, primarily influencing adrenergic signaling pathways. It exhibits low levels of adenylate cyclase inhibition in platelet membranes and enhances ADP-induced platelet aggregation with an EC50 of 1.5 μM. This compound is useful for research applications focusing on adrenergic receptor physiology and platelet function.

    10 mg
    $60.00
    25 mg
    $90.00
    All 2 sizes
  • L-749372
    Cat. No.
    A58529

    L-749372

    L-749372 is a selective partial agonist of the beta 3 adrenergic receptor, exhibiting an EC50 of 3.6 nM. This compound is instrumental in studying the modulation of metabolic processes and thermogenesis associated with beta 3 adrenergic receptor activity. Its unique properties make it a valuable tool for exploring obesity, metabolic disorders, and related therapeutic avenues in chemical research.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Prenalterol hydrochloride
    Cat. No.
    A58654

    Prenalterol hydrochloride

    Prenalterol hydrochloride is a selective partial agonist of the β1-adrenergic receptor, known for its positive inotropic effects. This compound has demonstrated significant efficacy in the management of acute heart failure, low output syndrome following myocardial infarction, and shock. Additionally, it has been used to alleviate orthostatic hypotension associated with Shy-Drager syndrome, making it a valuable reagent for cardiovascular research.

    25 mg
    $1,530.00
    50 mg
    $1,950.00
    All 3 sizes
  • BFE-55
    Cat. No.
    A58749

    BFE-55

    BFE-55 is a derivative of befunolol that acts as a β-adrenergic receptor partial agonist. This compound exhibits significant biological activity by modulating adrenergic signaling pathways. BFE-55 can be utilized in research focused on cardiovascular dynamics and therapeutic interventions targeting adrenergic receptors.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Cicloprolol hydrochloride
    Cat. No.
    A58814

    Cicloprolol hydrochloride

    Cicloprolol hydrochloride is a partial agonist of the β1-adrenergic receptor. It exhibits cardiovascular effects through the modulation of heart rate and contractility, making it a valuable tool in studies related to hypertension and heart failure. This compound is useful for investigating adrenergic receptor signaling and the physiological responses associated with β1-adrenergic activation.

    1 mg
    $560.00
    5 mg
    $1,475.00
    All 2 sizes
  • Epanolol
    Cat. No.
    A58852

    Epanolol

    Synonyms: Visacor; ICI141292

    Epanolol is a selective β-adrenoceptor partial agonist, demonstrating a higher affinity for β1-adrenoceptors compared to β2-adrenoceptors. This compound exhibits significant cardiovascular effects, making it useful in research focused on heart-related therapies and the modulation of adrenergic signaling pathways. Its specificity for β1-adrenergic receptors lends valuable insight into cardiac function and potential treatments for hypertension and other cardiovascular diseases.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

8 Items

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