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.

10 Items

  • CYD-1-79
    Cat. No.
    A29735

    CYD-1-79

    CYD-1-79 is a selective positive allosteric modulator of the 5-HT2C receptor. This compound enhances 5-HT-induced intracellular calcium release through a distinct allosteric site, demonstrating significant inhibition at dopamine D3 receptors, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 has been shown to modulate spontaneous ambulation in rodents and can synergize with low doses of 5-HT2C receptor agonists. Additionally, it reduces relapse vulnerability in models of psychoactive substance self-administration, highlighting its potential applications in neurological disease research.

    Out of stock

    All 3 sizes
  • Ipsapirone hydrochloride
    Cat. No.
    A29936

    Ipsapirone hydrochloride

    Synonyms: TVX Q 7821

    Ipsapirone hydrochloride is a selective modulator of the 5-HT1A receptor, functioning primarily as a partial agonist. This compound demonstrates anxiolytic properties, making it relevant for research in anxiety disorders. At elevated concentrations, ipsapirone hydrochloride can also exhibit antagonistic effects on the 5-HT1A receptor and inhibit 5-HT2 and α1-adrenergic receptor activities, expanding its applicability in pharmacological studies of serotonergic and adrenergic signaling pathways.

    5 mg
    $235.00
    10 mg
    $335.00
    All 3 sizes
  • Lubabegron
    Cat. No.
    A58140

    Lubabegron

    Synonyms: LY-488756

    Lubabegron is a potent modulator of β-adrenergic receptors (β-AR). It exhibits antagonistic activity at the β1 and β2 receptor subtypes while acting as an agonist for the β3 receptor subtype in cattle. This compound is effective in reducing ammonia gas emissions from livestock and their waste, making it relevant for environmental and agricultural research applications. Lubabegron holds potential for studies focusing on animal physiology and sustainable farming practices.

    5 mg
    $285.00
    10 mg
    $505.00
    All 5 sizes
  • Meranzin
    Cat. No.
    A58280

    Meranzin

    Meranzin is an adrenergic receptor modulator derived from the Traditional Chinese Medicine Chaihu-Shugan-San (CSS), isolated from the leaves of Murraya exotica L. It primarily regulates the alpha 2-adrenoceptor and influences the AMPA-ERK1/2-BDNF signaling pathway. Meranzin exhibits potential beneficial effects in preventing the co-occurrence of atherosclerosis and depression, making it a valuable tool for research in neurovascular health and related disorders.

    1 mg
    $85.00
    5 mg
    $225.00
    All 5 sizes
  • AP-7-168
    Cat. No.
    A58454

    AP-7-168

    AP-7-168 is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). It functions by promoting β2AR homodimerization and inhibiting GRK5-mediated phosphorylation, thereby sustaining bronchorelaxation in both cell and tissue models. This compound is particularly valuable for research in inflammation and immunology, including studies related to asthma and other respiratory conditions.

    Out of stock

    All 3 sizes
  • Arrestin-3 modulator-1
    Cat. No.
    A58670

    Arrestin-3 modulator-1

    Arrestin-3 modulator-1 is a selective modulator that interacts with arrestin-3 at the interdomain interface. This compound enhances the recruitment of arrestin-3 to phosphorylation-deficient β2-adrenergic receptors, as evidenced by increased Förster resonance energy transfer (FRET) levels in cellular assays. Arrestin-3 modulator-1 is valuable for studying congenital disorders such as retinal degeneration, hyperthyroidism, and obesity, offering insights into the molecular mechanisms underlying these conditions.

    Out of stock

    All 3 sizes
  • α1 adrenoceptor-MO-1
    Cat. No.
    A58850

    α1 adrenoceptor-MO-1

    α1 adrenoceptor-MO-1 is an S enantiomer that selectively targets the alpha-1 adrenergic receptor. This compound exhibits alpha-lytic activity and demonstrates analgesic properties, making it more effective than its R enantiomer counterpart. α1 adrenoceptor-MO-1 is suitable for research applications focused on adrenergic signaling and pain modulation.

    1 mg
    $165.00
    5 mg
    $340.00
    All 7 sizes
  • GP2-114
    Cat. No.
    A58857

    GP2-114

    GP2-114 is a selective adrenergic receptor modulator that exhibits current-dependent cardiovascular effects. It is utilized in experimental models to study the physiological impacts on cardiovascular function and adrenergic signaling pathways. The compound offers valuable insights into the role of adrenergic receptors in cardiovascular responses, supporting various research applications in pharmacology and cardiovascular physiology.

    1 mg
    $525.00
    5 mg
    $1,050.00
    All 6 sizes
  • Lubabegron fumarate
    Cat. No.
    A84964

    Lubabegron fumarate

    Synonyms: LY-591281; LY-488756 fumarate

    Lubabegron fumarate is a selectiveβ-adrenergic receptor (β-AR) modulator, exhibiting antagonistic properties at both β1 and β2 receptor subtypes while acting as an agonist at the β3 subtype in bovine species. This compound effectively reduces ammonia (NH3) gas emissions from livestock and their waste, making it a valuable tool for improving environmental sustainability in agricultural practices. Lubabegron fumarate is primarily used in research applications focused on animal health and emissions management.

    5 mg
    $285.00
    10 mg
    $505.00
    All 5 sizes
  • Fepradinol
    Cat. No.
    A96786

    Fepradinol

    Fepradinol is a drug derivative that primarily acts as a selective modulator of adrenergic receptors. This compound exhibits significant biological activity in influencing cardiovascular responses and can be utilized in research focused on cardiovascular pharmacology. Its modulatory effects make it valuable for investigating the therapeutic potential in treating various cardiovascular disorders.

    Out of stock

    All 3 sizes

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