GPCR/G Protein

Items 1301-1350 of 5455

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  1. antiplatelet activities

    6-Methoxydihydroavicine is an alkaloid isolated from Zanthoxylum integrifoliolum. 6-Methoxydihydroavicine has antiplatelet activities and inhibits AA-, collagen- and PAF-induced platelet aggregation in vitro.
  2. β1-adrenergic receptor antagonist

    Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias.
  3. 5-HT1B/1D receptor antagonis

    GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively.
  4. A1 adenosine receptor agonist

    Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury.
  5. SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties.
  6. allosteric inhibitor of CXCR1 and CXCR2

    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2.
  7. cannabinoid (CB2) agonist

    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  8. mGlu5 PAM

    ML-254, also known as VU0430644; is Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction.
  9. Salvinorin B is an analytical reference material categorized as a diterpene.

  10. β-adrenergic receptor (βAR) antagonist

    (R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively.

  11. β2-adrenergic agonist

    Clenproperol is a β2-adrenergic agonist.
  12. histamine H3R antagonist/inverse agonist

    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR.
  13. 5-HT3 receptor antagonist

    5-HT3 antagonist-4i is a 5-HT3 receptor antagonist which modulates the serotonergic system.
  14. CXCR4 antagonist

    Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ??1 nM.
  15. β2-AR agonist

    Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries.
  16. ODQ

    soluble guanylyl cyclase inhibitor

    ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
  17. analgesic agent

    Tetrahydropalmatine hydrochloride (DL-Tetrahydropalmatine hydrochloride), an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
  18. leukotriene B4 receptor antagonist

    Etalocib, also known as LY293111 and VML295, is a potent and selective inhibitor of the lipoxygenase pathway either directly through 5'-lipoxygenase or via antagonism of the leukotriene B4 (LTB4) receptor.
  19. melanocortin receptor (MR) agonist

    AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages.
  20. GLP-1R agonist

    PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R)
  21. 5-HT4 receptor partial agonist

    PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.
  22. 5-HT7 receptor antagonist

    AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders.
  23. mGlu1 receptor agonist

    Ro0711401 is a mGlu1 receptor agonist.
  24. 5-HT4 receptor antagonist

    SB203186 is potent 5-HT4 receptor antagonist.
  25. Melatonin receptor agonist

    ACH-000143 is a potent and peripherally preferred melatonin receptor agonist.
  26. 5-HT receptor agonist

    MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively).
  27. SEP-363856, also known as SEP-856, is an orally active and CNS active psychotropic agent.
  28. MT1/MT2 antagonist

    Luzindole, also known as N-0774, and N-acetyl-2-benzyltryptamine, is a melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values are = 10-27 and 158-513 nM, respectively).
  29. p75NTR modulator/proNGF antagonist

    LM11A-31 is a small-molecule p75NTR modulator and proNGF antagonist.
  30. prostaglandin synthase inhibitor

    Pizuglanstat is a hematopoietic prostaglandin synthase inhibitor.
  31. mGluR II agonist

    Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus.
  32. analgesic agent

    Tetrahydropalmatine, an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
  33. S1P2 antagonist

    JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively.
  34. dopamine D1-like receptor antagonist

    SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively.
  35. β-adrenergic receptor blocking agent

    Carazolol is a non-specific β-adrenergic receptor blocking agent and binds to β receptors irreversibly.
  36. 5-HT receptor agonist

    Quipazine maleate is a selective 5-HT receptor agonist that promotes the proliferation and apoptosis of human hepatocyte strain of L-02 strain and could also exert an excitatory effect on raphe neurons via stimulation of 5-HT2A receptors.
  37. agonist of FPR2/ALX

    ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes.
  38. angiotensin II receptor antagonist

    EMD-66684 is a non-peptide angiotensin II receptor antagonist.
  39. CB1/CB2 agonist

    NMP-7 is a non-selective agonist of the CB1 and CB2 cannabinoid receptors that acts by blocking T-type calcium channels.
  40. alpha2-Adrenergic receptor agonist

    Flutonidine is an alpha2-Adrenergic receptor agonist.
  41. mGluR1b antagonist

    CPCCOEt is a low affinity, selective, non-competitive antagonist of the metabotropic glutamate receptor subtype mGluR1b.
  42. mGlu1 receptorsant agonist

    YM 298198 is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM).

  43. group I mGlu antagonist

    NPS2390 is a group I mGlu antagonist. It displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors. NPS2390 is thought to act on a site separate from the glutamate binding pocket.
  44. Galanin receptors GALR agonist

    Galnon is a selective, non-peptide agonist at the galanin receptors GALR.
  45. pyrazolopyridine anxiolytic

    Tracazolate is a pyrazolopyridine anxiolytic known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases.
  46. Beta1-Adrenergic receptor antagonist

    Talinolol is a beta(1)-adrenergic receptor antagonist and a probe drug for P-glycoprotein (P-gp) activity in humans.

  47. histamine H1 receptor agonist and H3 receptor antagonist

    Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine. Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA).
  48. beta-adrenoceptor antagonist

    DL 071-IT is a potent non-selective beta-adrenoceptor antagonist. .
  49. PAM of mGluR4

    VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
  50. adenosine receptor antagonist

    AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities.

Items 1301-1350 of 5455

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