GPCR/G Protein

Items 451-500 of 6977

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  1. α2-receptor agonist

    Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.
  2. CCK antagonist

    Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. IProglumide is a known cholecystokinin (CCK) antagonist.
  3. sigma-2 (σ2) receptor ligand

    Glycerol phenylbutyrate is a sigma-2 (ς2) receptor ligand, with a pKi of 8.02.
  4. Histamine H1 antagonist

    Mequitazine is a potent histamine H1 antagonist or antihistamine. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract.
  5. alpha-1 adrenergic receptors / mAChRs inhibitor

    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
  6. Sodium deoxycholate is a bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.
  7. β2-adrenergic receptor agonist

    Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist.
  8. Somatostatin Receptor agonist

    Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).
  9. Bromperidol, also known as Impromen and R-11333, is used as a means of long-term maintenance treatment of schizophrenia. Bromperidol is a close structural analogue of haloperidol. C3435T polymorphism is associated with some therapeutic response to bromperidol in schizophrenic patients, possibly by different drug concentration in the brain.
  10. 5-HT receptor /dopamine receptors antagonist

    Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
  11. β-adrenergic receptor antagonist

    Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.
  12. Levomepromazine, also known as methotrimeprazine, is a phenothiazine neuroleptic drug. Levomepromazine is used for the treatment of psychosis, particularly those of schizophrenia, and manic phases of bipolar disorder.
  13. Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.
  14. Sincalide, also known as CCK-8, is a drug used to treat cholecystitis. Sincalide is an octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.
  15. dopamine D2 receptor antagonist

    Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.
  16. selective IP receptor agonist

    MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
  17. FFA4/GPR120 agonist

    TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism.
  18. α2 adrenoceptor antagonist

    Piperoxan hydrochloride is an α2 adrenoceptor antagonist.
  19. 5-HT1A receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone.
  20. EP4 agonist

    KAG-308, a newly-identified EP4-selective agonist shows efficacy for treating ulcerative colitis and can bring about lower risk of colorectal carcinogenesis by oral administration.
  21. ligand-linker conjugate

    CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker.
  22. S1P agonist

    ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively.
  23. NTR1 allosteric modulator

    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator.
  24. CRTH2 antagonist

    ACT-129968 is a potent and selective CRTH2 antagonist.
  25. vasopressin V1 antagonist

    OPC21268 is a non-peptide AVP Receptor V (Vasopressin Receptor) antagonist that shows 1000-fold selectivity for V1 receptors over V2 receptors.
  26. mGlu2 receptor modulator

    CBiPES hydrochloride is a selective positive allosteric modulator of the mGluR-2 with IC50 value of 98.2 nM
  27. mGluR5 Modulator

    VU0364289 is a novel N-aryl piperazine mGlu5 positive allosteric modulator.
  28. SK2 modulator

    NS13001 is a selective SK2/3 modulator that acts as a potential therapeutic agent for treatment of SCA2 and possibly other cerebellar ataxias.
  29. 5-HT1A/B/D receptor antagonist

    GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.
  30. Dopamine Receptor Agonist?€?

    SKF38393 HCl is a D1 agonist with IC50 of 110 nM.
  31. EGFR inhibitor

    Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.

     
  32. EP2 Agonist

    C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM.
  33. Serotonin2A Receptor Inverse Agonist

    Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson?€?s disease.
  34. A2A adenosine receptor antagonist

    SCH58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
  35. sGC activator?€?

    BAY 41-2272 is a direct and NO-independent soluble guanylate cyclase (sGC) stimulator.
  36. ETA receptor antagonist

    BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
  37. 5HT(1A) receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
  38. Nurr1 activator

    C-DIM12 is a novel synthetic activator of Nurr1. C-DIM12 induces dopaminergic gene expression and protects against 6-hydroxydopamine neurotoxicity in vitro.
  39. CXCR2 antagonist

    AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD.
  40. prostaglandin EP4 receptor antagonist

    Grapiprant is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties.
  41. Prostaglandin E2 receptor antagonist

    TG6-10-1 is a potent and selective antagonist for the prostaglandin E2 receptor subtype EP2.
  42. Opioid antagonist

    Naloxegol is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation.
  43. Orexin 2 receptor agonist

    A potent and selective Orexin2 receptor agonist.
  44. CysLT1 receptor antagonist

    MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively.
  45. CCK-2 receptor antagonist

    Nastorazepide is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
  46. β2-adrenergic receptor agonist

    Vilanterol is a long-acting beta-2 agonist drug, which in May 2013 was approved in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD).
  47. JMV 390-1 is a inhibitor of the major neurotensin and neuromedin N degrading enzymes (IC50 values are 31, 40, 52 and 58 nM for endopeptidase 24.15, endopeptidase 24.11, leucine aminopeptidase and endopeptidase 24.16 respectively).
  48. cAMPS-Sp, triethylammonium salt is a cell-permeable cAMP analog that activates cAMP receptor proteins such as PKA and cAMP-regulated guanine nucleotide exchange factor.
  49. dopaminergic stabilizer

    ACR 16 hydrochloride is a dopaminergic stabilizer (Ki values 17550 nM and 7521 for D2(low) and D2(high), respectively) that state-dependently stabilizes psychomotor activity by the dual actions of functional dopamine D2 receptor antagonism and strengthening of cortical glutamate functions in various settings of perturbed neurotransmission.
  50. Adenosine A1-R antagonist

    DPCPX, a xanthine derivative, is a very potent and selective Adenosine A1-R antagonist. It displays very modest efficacy against Adenosine A2A-R, Adenosine A2B-R and Adenosine A3-R.

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