GPCR/G Protein

Items 151-200 of 1393

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  1. A2a receptor antagonist

    SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders.
  2. ETA receptor antagonist

    Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively.
  3. ETA receptor antagonist

    Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure.
  4. OX Receptor Antagonist

    SB-408124 is a selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.
  5. Dopamine receptor ligand

    ST-836 is a dopamine receptor ligand; Antiparkinsonian agent.
  6. 5-HT6 receptor antagonist

    SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
  7. SIRT1 activator

    SRT3190 is a potent CXCR2 ligand.
  8. CB1 receptor inverse agonist

    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
  9. vasopressin receptor 2 antagonist

    Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM.
  10. Tianeptine is a selective facilitator of 5-HT uptake in vitro and in vivo.
  11. serotonin transporter (SER) inhibitor

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  12. LTD4 receptor antagonist

    Verlukast (MK-0679) is a potent leukotriene D4 antagonist
  13. Adenosine A2A Receptor Agonist

    CGS 21680 is a specific adenosine A2A subtype receptor agonist.
  14. α1-adrenergic receptor agonist

    Phenylephrine is a selective α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure.
  15. DL-Adrenaline is a hormone and a neurotransmitter secreted by the medulla of the adrenal glands. DL-Adrenaline is found in small amounts in the body and is essential for maintaining cardiovascular homeostasis because of its ability to divert blood to tissues under stress.
  16. CaSR agonist

    Strontium ranelate is an antiosteoporotic agent which both increases bone formation and reduces bone resorption, resulting in a rebalance of bone turnover in favor of bone formation. This is similar to the effects of choline stabilized orthosilicic acid.
  17. Brompheniramine is a first-generation antihistamine. Brompheniramine works by acting as an antagonist of histamine H1 receptors. It also functions as a moderately effective anticholinergic agent, and is likely an antimuscarinic agent similar to other common antihistamines such as diphenhydramine.
  18. Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic (to treat nausea and vomiting). Ondansetron reduces the activity of the vagus nerve, which deactivates the vomiting center in the medulla oblongata, and also blocks serotonin receptors in the chemoreceptor trigger zone.
  19. Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA) . Structurally, mirtazapine can also be classified as a tetracyclic antidepressant (TeCA).
  20. Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor (SARI) class. It is a phenylpiperazine compound. Trazodone also has anti-anxiety (anxiolytic) and sleep-inducing (hypnotic) effects.
  21. Urapidil hydrochloride is an α1-adrenoceptor antagonist, 5-HT1A serotonin receptor partial agonist and anti-hypertensive.
  22. Duloxetine is a serotonin-norepinephrine reuptake inhibitor (SNRI). It is effective for major depressive disorder and generalized anxiety disorder (GAD).
  23. histamine receptor antagonist

    Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM.
  24. NMDA receptor antagonist

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
  25. Beta1 receptor blocker

    Metoprolol is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.
  26. H2 receptor antagonist

    Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action.
  27. Duloxetine Hydrochloride is a dual serotonin and norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of stress urinary incontinence, as well as depression.
  28. Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects.
  29. Fenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive crisis.
  30. Betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and glaucoma. Being selective for beta1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta2 receptors) as timolol may. Betaxolol also shows greater affininty for beta1 receptors than metoprolol.
  31. Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H1 receptors.
  32. Formoterol is a long-acting β2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD).
  33. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
  34. Phentolamine is a reversible nonselective alpha-adrenergic antagonist.
  35. Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH).
  36. imidazoline receptor 1 agonist

    Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). Moxonidine causes a decrease in sympathetic nervous system activity and, therefore, a decrease in blood pressure.
  37. Thromboxane A2 synthesis inhibitor

    Ozagrel is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor.
  38. 5-HT antagonist

    Tegaserod functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist.
  39. mGluR5 PAM

    VU 0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax.
  40. neurokinin-1 receptor antagonist

    Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.
  41. Prostaglandin D2 receptor CRTH2 antagonist

    CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist.
  42. CCK-A receptor antagonist

    Loxiglumide (CR1505) is a cholecystokinin antagonist
  43. NT Antagonist

    SR 48692 represents a new, potent, nonpeptide antagonist radioligand of the NT receptor that differentiates between agonist- and antagonist-receptor interactions.
  44. 5-HT Receptor agonist

    Prucalopride is a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements.
  45. AT1 Receptor Blocker

    Azilsartan (TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension.
  46. CB2 agonist

    JWH-133 is a potent selective CB2 receptor agonist, with a Ki of 3.4nM and selectivity of around 200x for CB2 over CB1 receptors.
  47. beta2-adrenergic receptor agonist

    Salmeterol is a long-acting beta2-adrenergic receptor agonist
  48. PGF2α/LTB4 production inhibitor

    Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
  49. 5-HT Receptor agonist

    Almotriptan malate (Axert) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.

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