GPCR/G Protein

Items 501-550 of 6977

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. H4 receptor antagonist

    JNJ-39758979 is histamine H4 receptor antagonists with a Ki of 12.5 nM.
  2. GPR39 agonist

    TM N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.
  3. α1 adrenoreceptor antagonist

    Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.
  4. 5-HT(2A) receptor agonist

    Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis.
  5. EP1 receptor antagonist

    GSK-269984A is a novel EP1 receptor antagonist.
  6. opioid receptor antagonis

    Bevenopran, also known as CB-5945, ADL-5945, MK-2402, OpRA III, is a peripherally selective μ- and δ-opioid receptor antagonist.
  7. Neuronostatin-13 human is a 13-amino acid peptide hormone encoded by the somatostatin gene and plays an important role in the regulation of hormonal and cardiac function.
  8. Rev-Erbα agonist

    GSK4112 is a selective Rev-Erbα agonist with EC50 value of 250 nM.
  9. OX2 receptor antagonist

    TCS-OX2-29 is a selective OX2 receptor antagonist with IC50 value of 40 nM. CAS: 1610882-30-8 (HCl) 372523-75-6 (Free Base)
  10. IP (prostacyclin) receptor antagonist

    RO-1138452 is a potent and selective IP (prostacyclin) receptor antagonist with high affinity for IP receptors.
  11. sigma1 receptor agonist

    Anavex2-73 is a muscarinic/moderate sigma1 receptor agonist that alleviated the scopolamine- and dizocilpine-induced learning impairments. CAS: 195615-83-9 (Free base) 195615-84-0 (HCl)
  12. histamine H3 receptors agonist

    S38093 is an inverse agonist at histamine H3 receptors. CAS: 862896-30-8 (Free base) 1222097-72-4 (HCl)
  13. CXCR4 Antagonist

    MSX-130 is CXCR4 antagonist.
  14. CXCR4 receptor modulator

    NSC-23026 is a CXCR4 receptor modulator.
  15. GPCR19 antagonist

    SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
  16. CRTh2 receptor antagonist

    Fevipiprant, also known as NVP-QAW039 or QAW039, is an oral active and potent CRTh2 receptor antagonist and potentially useful for asthma treatment.
  17. beta-adrenergic receptor antagonist

    Nifenalol, also known as INPEA, is a new beta-adrenergic receptor antagonist.
  18. α-adrenoceptor agonist

    Xylometazoline hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant.
  19. alpha-adrenergic receptor agonist / MAO inhibitor

    Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release.
  20. 5-HT2 antagonist

    Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.
  21. D2DR and D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia.
  22. MT1 and MT2 receptor agonist

    Tasimelteon is a melatonin MT1 and MT2 receptor agonist.
  23. β-adrenergic receptor antagonist

    (R)-Atenolol is a beta blocker used to treat high blood pressure and chest pain (angina). It can also reduce the risk of death after a heart attack.
  24. β2AR agonist

    Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.
  25. alpha-1 adrenergic agonist

    Methoxamine Hydrochloride is an alpha-1 adrenergic agonist that causes prolonged peripheral vasoconstriction.
  26. Non-selective β antagonist

    Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively).
  27. beta-Adrenergic agonist

    Ractopamine HCl is a beta-Adrenergic agonist. It acts by being a full agonist at the TAAR1.
  28. H1 histamine receptor antagonist

    Terfenadine ((??)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 and induces p73, Noxa.
  29. Dopamine receptor antagonist

    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  30. Misoprostol is a medication used to start labor, cause an abortion, prevent and treat stomach ulcers, and treat postpartum bleeding due to poor contraction of the uterus. For abortions it is often used with mifepristone or methotrexate. By itself effectiveness for this purpose is between 66% and 90%.
  31. 5-HT3 receptor antagonist

    Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist.
  32. α1A-adrenoceptor antagonist

    Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has been found to increase mental agility and enhance clarity and perception. It decreases vascular resistance and increases arterial blood flow in the brain, improving the utilization of oxygen and glucose by brain cells. It has similar vasoactive properties in other areas of the body, particularly the lungs. Nicergoline is used for vascular disorders such as cerebral thrombosis and atherosclerosis, arterial blockages in the limbs, Raynaud's disease, vascular migraines, and retinopathy.
  33. Histamine H1 receptor antagonist

    Levocetirizine dihydrochloride is a L-isomer of cetirizine and histamine H1 receptor antagonist. It incrases levels of CD4+ CD25+ T cells and decreases levels of eosinophils, decreasing allergy symptoms.
  34. prostaglandin analogue

    Tafluprost, also known as MK2452 and AFP-168, is a prostaglandin analogue used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.
  35. non-peptide angiotensin II receptor antagonist

    Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys.
  36. beta Adrenergic Receptor blocker

    Nadolol is a non-selective beta blocker used in the treatment of high blood pressure and chest pain. Additionally, it is often prescribed in the treatment of atrial fibrillation, migraine headaches, and complications of cirrhosis.
  37. Dopamine D1/2 receptor antagonist

    Melitracen HCl ia potential dopamine D1/2 receptor antagonist used to treat depression. It is often co-administered with flupenthixol as a treatment for trigeminal neuralgia. It does not effect cardiovascular function.
  38. Prostaglandin Receptor inhibitor

    Benorilate, also known as Win-11450, is an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases. Benorilate has less severe side effects than aspirin.
  39. Prostaglandin Receptor inhibitor

    Dinoprost Tromethamine, also known as Dinoprost Trometamol, is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
  40. Angiotensin II receptor antagonist

    Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
  41. Carbazochrome, also known as Adona and AC-17, is a hemostatic which increases capillary resistance and activates platelet factors.
  42. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  43. 5-HT3 receptor antagonist

    Dolasetron is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness.
  44. 5-HT2 receptors inhibitor

    Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test.
  45. D2DR inhibitor

    Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity.
  46. MAO inhibitor

    Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor.
  47. D2 receptor blocker

    Trimethobenzamide hydrochloride is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
  48. adrenoceptor antagonist

    Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity?=?255:1, a half-life of 4?min)?? acts as an adrenoceptor antagonist.
  49. histamine H1 receptor antagonist

    Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. This medication is an antihistamine, prescribed for allergic conjunctivitis.
  50. Histamine H1 receptor antagonist

    Hydroxyzine pamoate is an histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness.

Items 501-550 of 6977

Page
per page
Set Descending Direction