GPCR/G Protein

Items 5601-5650 of 6977

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Catalog No.
Product Name
Application
Product Information
Citations
  1. H1 histamine receptor antagonist

    Clemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding.
  2. mGluR1 modulator

    CPPHA is a selective positive allosteric modulator of mGluR5 receptor.
  3. dopamine agonist

    Dexpramipexole dihydrochloride is a neuroprotective agent and weak non-ergoline dopamine agonist.
  4. H2-receptor antagonist

    Ebrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection.
  5. GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
  6. GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
  7. 5-HT3 antagonist

    Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  8. α2A-adrenoceptor agonist

    Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.
  9. Metabolites of tulobuterol

    HOKU-81, a new bronchodilator, is one of the metabolites of tulobuterol.
  10. 5HT1F agonist

    LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
  11. k-opioid receptor antagonist

    LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.
  12. μ-opioid antagonist

    Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.
  13. Dopamine Receptor antagonist

    Metoclopramide is a dopamine D2 antagonist that is used as an antiemetic.
  14. CGRP Receptor antagonist

    MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
  15. mGlu5 antagonist

    MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively.
  16. NK1 receptor antagonist

    NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.
  17. Noopept is a medication promoted and prescribed in Russia and neighbouring countries as a nootropic.
  18. CB1 receptor antagonist

    Otenabant is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.
  19. Dopamine reuptake inhibitor

    Phenylpiracetam is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam.
  20. Nonimidazole inverse agonist

    Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
  21. Nonimidazole inverse agonist

    Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
  22. Quetiapine is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.
  23. D2 receptor agonist

    rac-Rotigotine Hydrochloride is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM.
  24. CXCL8 receptor inhibitor

    Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.
  25. NK3 receptor antagonist

    SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.
  26. OX Receptor Antagonist

    SB408124 Hcl is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.
  27. OX1 receptor antagonist

    SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.
  28. ST-836 Hcl is a dopamine receptor ligand; Antiparkinsonian agent.
  29. NK3 receptor antagonist

    Talnetant is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.
  30. NK3 receptor antagonist

    Talnetant Hcl is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.
  31. 5HT1A antagonist

    WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 - 0.12 nM for 5-HT.
  32. H2-receptor antagonist

    Zaltidine is a H2-receptor antagonist, which has the antisecretory action.
  33. 5-HT/dopamine receptor antagonist

    Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  34. LTA4 hydrolase Inhibitor

    SC 57461A is a potent and competitive inhibitor of recombinant human leukotriene A4 hydrolase in vitro (Askonas et al., 2002).
  35. LPA2 agonist

    GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM).
  36. mGluR1 antagonist

    DL-AP3, a racemic preparation of D-AP3 and L-AP3, is an inhibitor of phosphoserine phosphatase and an antagonist of the metabotropic glutamate receptor (mGluR), blocking phosphoinositide turnover mediated by the mGluR.
  37. 5-HT Receptor Antagonist

    SB271046 is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.
  38. CXCL chemokines antagonist

    UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.
  39. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  40. EGFR inhibitor

    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
  41. serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  42. 5-HT3 receptor antagonist

    Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.
  43. 5-HT3 antagonist

    LY278584 is a potent and selective antagonist of 5-HT3 receptors. LY278584 is a useful ligand for studying the localization of 5-HT3 receptors in rat brain
  44. 5HT3 receptor antagonist

    Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity.
  45. NA reuptake inhibitor

    MCI-225 is a selective NA reuptake inhibitor with 5-HT3 receptor antagonism.
  46. EP4 receptor antagonist

    GW627368 is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor(Ki= 100 nM) with additional human TP receptor affinity(Ki= 150 nM).
  47. EP4 receptor antagonist

    MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, displayed strong binding affinity for the EP4 receptor with Ki of 0.7 nM,
  48. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.
  49. 5-HT1E/5-HT1F receptor agonist

    BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
  50. 5-HT3 receptor inhibitor

    Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.

Items 5601-5650 of 6977

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