GPCR/G Protein

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  1. vasoconstrictor

    Terlipressin is a potent vasoconstrictor that acts via V1 receptors on arteriolar smooth muscle cells.
  2. Angiotensin II human is a vasoconstrictor that acts on the AT1 and the AT2 receptor.
  3. histamine H1-receptor antagonist

    Diazoline is a histamine H1-receptor antagonist.
  4. adrenergic receptor inhibitor

    Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  5. histamine H1 antagonist

    Chlorcyclizine hydrochloride is a histamine H1 antagonist.
  6. dopamine D2 receptor agonist

    Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.
  7. β-adrenergic receptor antagonist

    Metipranolol (hydrochloride) is a non-selective β-adrenergic receptor (β-AR) antagonist. Formulations containing metipranolol have been used in the treatment of elevated IOP in patients with ocular hypertension or glaucoma.
  8. Dopamine D2 antagonist

    Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic.
  9. D2DR/D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  10. Bradykinin B2 receptors antagonist

    Icatibant (HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.
  11. peripheral oxytocin receptors agonist

    Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.
  12. 5-HT receptor antagonist

    Pizotifen is a serotonin antagonist which acts mainly at the 5-HT1, 5-HT2A, and 5HT2C receptors with some antihistamine activity.
  13. DOPA decarboxylase inhibitor

    Methyldopa Sesquihydrate is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension.
  14. μ- opioid receptor agonist

    Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome.
  15. thromboxane A2 (TXA2) receptor (TP receptor) antagonist

    Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma.
  16. 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.
  17. 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.
  18. sigma-2 (σ2) receptor ligand

    Glycerol phenylbutyrate is a sigma-2 (ς2) receptor ligand, with a pKi of 8.02.
  19. 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.
  20. alpha-1 adrenergic receptors / mAChRs inhibitor

    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
  21. 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.
  22. β2-adrenergic receptor agonist

    Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist.
  23. 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).
  24. 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.
  25. 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.
  26. β-adrenergic receptor antagonist

    Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.
  27. 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.
  28. 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.
  29. 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.
  30. dopamine D2 receptor antagonist

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

    MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
  32. 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.
  33. α2 adrenoceptor antagonist

    Piperoxan hydrochloride is an α2 adrenoceptor antagonist.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. NTR1 allosteric modulator

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

    ACT-129968 is a potent and selective CRTH2 antagonist.
  40. 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.
  41. mGlu2 receptor modulator

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

    VU0364289 is a novel N-aryl piperazine mGlu5 positive allosteric modulator.
  43. 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.
  44. 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.
  45. Dopamine Receptor Agonist?€?

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

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

     
  47. EP2 Agonist

    C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM.
  48. 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.
  49. 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.
  50. sGC activator?€?

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

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