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Results for "

competitive antagonism

" in MedChemExpress (MCE) Product Catalog:

9

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-113906A
    (αR,8aS)-GSK1614343

    		GHSR Metabolic Disease
    (αR,8aS)-GSK1614343 is the isomer of GSK1614343 (HY-113906). GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors .
    (αR,8aS)-GSK1614343
  • HY-117694
    MK-8825

    		CGRP Receptor Neurological Disease Inflammation/Immunology
    MK-8825 is an orally active, selective CGRP receptor antagonist with a Ki value of 47 pM for human CGRP receptors and 17 nM for rat CGRP receptors. MK-8825 blocks CGRP-stimulated cAMP responses and exhibits competitive-like antagonism. MK-8825 can be used in the research of migraine and temporomandibular joint disorders .
    MK-8825
  • HY-N7740
    Adenosine 2',5'-diphosphate sodium

    		P2Y Receptor Endogenous Metabolite Others
    Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors .
    Adenosine 2',5'-diphosphate sodium
  • HY-135439
    SB-203186

    		5-HT Receptor Neurological Disease
    SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .
    SB-203186
  • HY-19012
    N-1518

    		Adrenergic Receptor Cardiovascular Disease
    N-1518 is an α and β adrenergic receptor blocker that has competitive antagonism against β1 and α1 receptors, but does not show selectivity for β1 receptors, but shows about 20-fold selectivity for α1 receptors. N-1518 has vasodilatory effects and can be used in the research field of hypertension treatment .
    N-1518
  • HY-W424730
    HA-966 hydrochloride

    		iGluR Others
    HA-966 hydrochloride is a glycine site antagonist of the NMDA receptor, exhibiting non-competitive antagonism on NMDA responses. HA-966 hydrochloride effectively blocks the enhancement of NMDA responses by glycine in a competitive manner. HA-966 hydrochloride plays a significant role in mediating the antagonist action at the glycine modulatory site of the NMDA receptor.
    HA-966 hydrochloride
  • HY-19633A
    CS-003

    		Endogenous Metabolite Neurological Disease
    CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guinea pig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists .
    CS-003
  • HY-182427
    ORF 17583

    		Histamine Receptor Inflammation/Immunology
    ORF 17583 is a Ranitidine (HY-B0693) analogue and H2 receptor antagonist. ORF 17583 exhibits typical reversible competitive antagonism in the guinea pig right atria model, causing a dose-dependent rightward shift of the histamine concentration-response curve without reducing the maximum effect, and its action is fully reversible upon washing. ORF 17583 can be used for research on peptic ulcers and hyperacidity .
    ORF 17583
  • HY-182635
    ICI 147798

    		Adrenergic Receptor Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease
    ICI 147798 is an orally effective β-adrenoceptor antagonist with a pKB of 9.1 (in guinea pig right atrium) and 8.8 (in guinea pig trachea). ICI 147798 acts as a diuretic and intraocular pressure-lowering agent. ICI 147798 blocks β-adrenoceptors, inhibits isoproterenol-induced tachycardia and vasodepressor responses, exhibits slowly dissociating, insurmountable antagonism against β1-adrenoceptors, and shows surmountable competitive antagonism against β2-adrenoceptors. ICI 147798 induces natriuresis and kaliuresis, inhibits sodium transport, and reduces intraocular pressure .
    ICI 147798

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