GPCR/G Protein

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  1. β1-adrenergic receptor antagonist

    Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias.
  2. 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.

  3. histamine H3R antagonist/inverse agonist

    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR.
  4. 5-HT3 receptor antagonist

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

    Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ??1 nM.
  6. 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.
  7. 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.
  8. 5-HT4 receptor antagonist

    SB203186 is potent 5-HT4 receptor antagonist.
  9. 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).
  10. p75NTR modulator/proNGF antagonist

    LM11A-31 is a small-molecule p75NTR modulator and proNGF antagonist.
  11. 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.
  12. 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.
  13. angiotensin II receptor antagonist

    EMD-66684 is a non-peptide angiotensin II receptor antagonist.
  14. mGluR1b antagonist

    CPCCOEt is a low affinity, selective, non-competitive antagonist of the metabotropic glutamate receptor subtype mGluR1b.
  15. 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.
  16. Beta1-Adrenergic receptor antagonist

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

  17. 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).
  18. beta-adrenoceptor antagonist

    DL 071-IT is a potent non-selective beta-adrenoceptor antagonist. .
  19. 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.
  20. antagonist of histamine H1

    Cyclizine is an antagonist of histamine H1. Cyclizine is an antihistamine drug that can be used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operatively following administration of general anaesthesia and opioids.
  21. GLP-1 antagonist

    Avexitide (Exendin (9-39)) is a specific and competitive GLP-1 receptor antagonist.
  22. vasopressin/oxytocin receptor antagonist

    Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.
  23. MC3/4R Antagonist

    SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
  24. vasopressin antagonist

    Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
  25. NK2 receptor peptide antagonist

    GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.
  26. somatostatin receptor 2 antagonist

    DOTA-JR11 is a somatostatin receptor 2 (SSTR2) antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research.

  27. bradykinin B1 receptor antagonist

    R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin-diabetic mice.

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