GPCR/G Protein

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  1. α2- adrenoceptor antagonist / I2 imidazoline receptor agonist

    Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively).
  2. imidazoline receptor 1 agonist

    Moxonidine hydrochloride is a centrally acting antihypertensive agent.
  3. 5-HT1A receptor antagonist

    NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor.
  4. Octopamine hydrochloride is an invertebrate biogenic amine neurotransmitter, related to noradrenalin, that is an adrenoceptor agonist.
  5. α-Adrenergic blocker

    Phentolamine Hydrochloride is an AR (α-Adrenergic) blocker.
  6. Beta adrenergic receptor blocker

    Pindolol is a nonselective beta blocker with partial beta-adrenergic receptor agonist activity.
  7. norepinephrine (NE) transporter inhibitor

    Atomoxetine hydrochloride is a competitive and specific inhibitor of SLC6A2 while demonstrating weak ST and DAT inhibition as studied in synaptosomes of rat hypothalamus.
  8. α2-adrenergic receptor antagonist

    Rauwolscine is a natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM).
  9. Adrenoceptors antagonist

    S-(-)-Atenolol is the active enantiomer of atenolol that is a cardioselective β-adrenergic blocker.
  10. Adrenoceptors antagonist

    (S)-Timolol maleate is a adrenergic receptor antagonist selective for β1-AR.
  11. Adrenoceptors antagonist

    SR 59230A hydrochloride is a β3-adrenoceptor antagonist.
  12. Adrenergic Receptor agonist

    Tulobuterol is a beta-adrenergic receptor agonist that is related structurally to Terbutaline.
  13. Adrenoceptors agonist

    UK 14,304 tartrate is a water-soluble form UK 14,304. It is a full α2 adrenergic agonist.
  14. Adrenergic Receptor agonist

    Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR.
  15. Histamine H4 receptor antagonist

    A 943931 2HCl is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively).
  16. Somatostatin is an endogenous peptide noted to inhibit the release of growth hormone, insulin and glucagon.
  17. serotonin uptake inhibitor

    Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively).
  18. GPR40/FFA1 agonist

    AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist.
  19. δ opioid receptor agonist

    ADL5747 is a selective, nonpeptidic δ opioid receptor agonist.
  20. Kainate receptor agonist

    Kainate class of ionotropic glutamate receptor agonist. Has been shown to induce seizures and neurodegeneration in vivo and has also been used to induce experimental epilepsy in rodents and to examine excitation-induced neuronal apoptosis mechanisms.
  21. Bombesin is a neuropeptide with many biological effects including hormone release, stimulation of pancreatic enzyme secretion, inhibition of gastric emptying and modulation of gastric acid secretion.
  22. prostanoid DP-receptor (DP1) agonist

    BW 245C is a prostanoid DP-receptor (DP1) agonist, used to treat stroke.
  23. PAR1 inhibitor

    ML-161 is an inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets).
  24. prostaglandin F2α analog

    Cloprostenol is a synthetic analog of prostaglandin F2α (PGF2α). It is 200 times and 100 times more potent than PGF2α in terminating pregnancy in hamsters and rats, respectively, without the side effects associated with PGF2α.
  25. ETA/ETB antagonist

    PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively.
  26. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  27. Adenosine A2A receptor antagonist

    Preladenant is a potent and selective antagonist at the adenosine A2A receptor.
  28. Sigma2 antagonist

    UMB24 is a putative sigma2-preferring antagonist.
  29. D2 dopamine partial agonist

    Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD).
  30. CRF1 receptor antagonist

    R121919 is a potent small-molecule CRF1 receptor antagonist.
  31. NTR1 agonist

    ML-314 is a brain penetrant nonpeptidic β-arrestin biased ggonist of the neurotensin NTR1 receptor, which exhibits full agonist behavior against NTR1 (EC50 = 2.0 μM) in the primary assay and selectivity against NTR2.
  32. Adenylyl Cyclase Inhibitor

    NKY 80 is an inhibitor of adenylyl cyclase (AC). Exhibits greater affinity for AC5 over AC3 and AC2 (IC50 values are 8.3 μM, 132 μM and 1.7 mM respectively).
  33. Angiotensin AT1 receptor antagonist

    SL910102 is a nonpeptide angiotensin AT1 receptor antagonist.
  34. adrenergic receptor antagonist

    Celiprolol HCl is a b1 adrenergic receptor antagonist and a b2 adrenergic receptor partial agonist that has been shown to relax human arteries and veins with ED50 values of 40-50 M in vitro.
  35. 2A-AR adrenergic agonist

    Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand.
  36. EDG-1 (S1P1) agonist

    CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM).
  37. ETBR antagonist

    IRL-2500 is a potent, selective ETBR antagonist. It shows some selectivity for ETB receptors (IC50 values are 1.3 and 94 nM for ETB and ETA receptors respectively).
  38. histamine H3 receptor agonist

    Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively).
  39. human 5'-methylthioadenosine phosphorylase inhibitor

    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
  40. β3 adrenergic agonist

    CL 316243 disodium salt, a beta-3 adrenergic agonist, was developed as an anti-obesity and diabetes drug, and causes rapid decreases in blood glucose levels in mice.
  41. 5HT2A antagonist

    Ketanserin tartrate is a salt of Ketanserin. Ketanserin is reported to have a high affinity for multiple G protein-coupled receptors, such as serotonin receptors.
  42. guanylate cyclase (sGC) stimulator

    Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.
  43. CCK-2 receptor antagonist

    Z-360 is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
  44. dopamine β-hydroxylase (DBH) inhibitor

    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects.
  45. G15

    GPER/GPR30 antagonist

    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
  46. β3-adrenergic receptors agonist

    BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity.
  47. dopamine D3 Receptor (DRD3) antagonist

    GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.
  48. opioid receptors agonist

    DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively.
  49. dopamine D2 receptor agonist

    Bromocriptine mesylate is a potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM).1,2 As a result, it has found applications in combination therapy for Parkinsonism.
  50. CCK antagonist

    Proglumide sodium salt is a non-selective cholecystokinin (CCK) antagonist. It inhibits CCK-stimulated amylase secretion and prevents CCK-induced 2-deoxyglucose uptake in mouse pancreatic acini.

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