GPCR/G Protein

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  1. A1-Adenosine Antagonist

    Naxifylline is a potent and selective A1-adenosine antagonist, exhibiting Ki values of 0.67 nM for rat A1 receptors and 0.45 nM for cloned human A1 receptors. This compound serves as a potassium-sparing diuretic, making it useful for investigating edema related to congestive heart failure. Naxifylline's mechanism of action provides critical insights into adenosine receptor signaling and its implications in cardiovascular research.
  2. Hypnotic Agent

    YGZ-331 is a hypnotic agent that primarily targets adenosine receptors A1R and A2aR. It enhances GABA levels and exerts a sedative-hypnotic effect by inhibiting the phosphorylation of CaMKII (pCaMKII). This compound has demonstrated the ability to reduce spontaneous motor activity in mice, making it a valuable tool for research into sedative mechanisms and sleep-related studies.
  3. A2A/A3 AR Antagonist

    A2A/A3 AR antagonist-1 is a dual antagonist of the human A2A and A3 adenosine receptors, exhibiting dissociation constants (Kis) of 90 nM and 31.8 nM for hA2A AR and hA3 AR, respectively. This compound serves as a fluorescent ligand, facilitating the study of adenosine receptor signaling pathways. Its biological activity makes it a valuable tool for research applications in pharmacology, receptor biology, and the development of therapies targeting adenosine-related disorders.
  4. Adenosine A1 Receptor Antagonist

    NPC 200 is a potent and selective antagonist of the Adenosine A1 receptor. It effectively reverses NECA-induced left and right atrial depression, demonstrating EC50 values of 1.08 and 2.03 μM, respectively. This compound is valuable for research into cardiovascular function and the role of adenosine receptors in various physiological processes.
  5. Adenosine Receptor Agonist

    Adenosine Receptor Agonist 2 is a potent adenosine A2B receptor (A2BR) agonist with an EC50 of 0.38 nM. This compound effectively inhibits the accumulation of cyclic AMP (cAMP) and calcium, demonstrating its role in modulating intracellular signaling pathways. Adenosine Receptor Agonist 2 is suitable for research applications focused on cardioprotection and related cardiovascular studies.
  6. A1/A3 Antagonist

    A1/A3 AR antagonist 1 is a potent dual antagonist of the adenosine A1 and A3 receptors, exhibiting affinity constants (Kis) of 36.7 nM for human A1, 25.4 nM for human A3, and 1.47 nM for rat A1. This compound is valuable for investigating various biological processes, particularly in the context of kidney failure, inflammatory pulmonary diseases, and Alzheimer's disease. Its dual receptor targeting makes it a useful tool for exploring the roles of adenosine receptors in these conditions.
  7. Adenosine Receptor Antagonist

    Xanthine amine congener dihydrochloride is a potent antagonist of adenosine A1 and A2 receptors, exhibiting IC50 values of 1.8 nM and 114 nM, respectively. This compound has demonstrated convulsant activity in murine models, making it a valuable tool for studying adenosine receptor involvement in neurological research and potential therapeutic applications. Its selectivity and potency make it suitable for investigations into the modulation of adenosine signaling and its implications in various physiological processes.
  8. A1 Adenosine Receptor Antagonist

    IRFI-165 is a potent and selective antagonist of the A1 adenosine receptor, exhibiting a Ki value of 7.9 nM for the rat A1 adenosine receptor. This compound shows a high degree of selectivity over A2A and A3 receptors. IRFI-165 has demonstrated antidepressant activity in vivo, making it a valuable tool for studying psychiatric and neurological disorders in research applications.
  9. A1AR Antagonist

    FSCPX is a potent and selective irreversible antagonist of the A1 adenosine receptor (A1AR), exhibiting low nanomolar affinity for this target. By effectively reducing interstitial adenosine levels, FSCPX can alter the impact of nucleoside transport inhibitors such as NBTI in cardiac tissue. This compound is valuable for research applications focused on cardiovascular pharmacology and adenosine signaling pathways.
  10. Adenosine Receptor Antagonist

    Adenosine receptor antagonist 1 is a selective antagonist for the A2A adenosine receptor, exhibiting an IC50 of 0.29 nM. This compound demonstrates a 14-fold greater selectivity for A2A receptors compared to A2B receptors. It is widely used in research to investigate the modulatory effects of adenosine signaling in various physiological and pathological processes.
  11. Adenosine Receptor antagonist

    N-0861 is a selective antagonist of the A1 adenosine receptor. It effectively inhibits the negative conduction effects associated with adenosine, such as prolonged AH interval and chest pain, without significantly affecting the increase in coronary blood flow velocity induced by adenosine. This specificity makes N-0861 a valuable tool for research in cardiovascular physiology and the exploration of adenosine receptor signaling pathways.
  12. Adenosine Analog

    8-Methoxyadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory effects and possesses potential anti-cancer properties by inhibiting tumor progression. It is valuable for research applications in cardiovascular studies and cancer biology, providing insights into adenosine's role in these processes.
  13. mGlu5 Agonist

    VU0424465 is a potent partial agonist and positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5), primarily targeting intracellular calcium (iCa2+) mobilization. With a Ki value of 11.8 nM, VU0424465 demonstrates high affinity at the MPEP allosteric binding site. This compound also facilitates the activation of pERK1/2 in cortical neurons, making it a valuable tool for research into neurological disorders and signaling pathways associated with mGlu5 activation.
  14. D3R PAM-Antagonist

    MLS6357, a D3 dopamine receptor (D3R)-selective positive allosteric modulator and antagonist, demonstrates significant antagonist activity in D3R-mediated assays, including BRET-based β-arrestin recruitment and Go-BRET assays, with IC50 values of 13 μM, 14 μM, and 17 μM respectively. It shows selectivity for D3R, with no notable activity on other dopamine receptor subtypes (D1R, D2R, D4R, D5R) at concentrations above 100 μM. MLS6357 serves as a valuable tool for investigating neuropsychiatric disorders, particularly in the context of substance use disorders.
  15. A2 Agonist

    CI-936 is an orally active A2 adenosine receptor agonist exhibiting an affinity of 25 nM. This compound demonstrates significant and selective activities in preclinical models associated with antipsychotic efficacy. Notably, CI-936 effectively inhibits exploratory behavior in mice, making it a valuable tool for understanding the neuropharmacological pathways linked to psychotropic effects.
  16. Adenosine Analog

    N6-Benzoyl-7'-O-DMT-morpholino adenine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits notable biological activities, including smooth muscle vasodilation and the potential inhibition of cancer progression. It is commonly utilized in research applications related to cardiovascular studies and cancer therapeutics, contributing valuable insights into adenosine signaling and its effects on physiological processes.
  17. Adenosine Analog

    2-Cyanomethylthioadenosine is an adenosine analog that primarily targets adenosine receptors. This compound demonstrates potent vasodilatory effects on smooth muscle tissue and has shown potential in inhibiting cancer progression. It serves as a valuable tool in research applications focusing on vascular biology and cancer therapeutics.
  18. Adenosine Analog

    3’-β-C-Ethynyladenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits smooth muscle vasodilatory effects and has been implicated in the inhibition of cancer progression. Additionally, this compound serves as a click chemistry reagent, featuring an alkyne group that allows it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation applications in chemical biology and drug development.
  19. Adenosine Analog

    7'-O-DMT-morpholino thymine is an adenosine analog primarily known for its role in modulating adenosine receptors. It exhibits biological activities such as smooth muscle vasodilation and may play a role in inhibiting cancer progression. This compound is valuable for research applications in cardiovascular studies and cancer biology, providing insights into cellular signaling pathways and therapeutic strategies.
  20. Adenosine Analog

    N6,N6-Dimethyl-2’-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects on smooth muscle and has been implicated in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular studies and cancer biology, providing insights into the modulation of adenosine signaling pathways.
  21. Adenosine Analog

    N6-(3-Methoxybenzyl)-2’-C-methyl adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant biological activity as a smooth muscle vasodilator and demonstrates potential anti-cancer properties. It is suitable for research applications focused on vascular biology and cancer therapeutics.
  22. Adenosine Analog

    N6-Methyl-2’-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound has demonstrated vasodilatory effects on smooth muscle and exhibits potential in inhibiting cancer progression. Its unique structure allows for various research applications related to adenosine signaling pathways and therapeutic interventions.
  23. Adenosine Analog

    5’-O-(4,4’-Dimethoxytrityl)-N6-phenoxyacetyl adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory effects and has been implicated in the inhibition of cancer progression. It is a valuable reagent for research focused on vascular biology, immunology, and oncology, facilitating investigations into the therapeutic potential of nucleotide derivatives.
  24. Adenosine Analog

    5'-O-[Bis(4-methoxyphenyl)phenylmethyl]-adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for cancer research. It serves as a useful tool in studies focused on adenosine receptor modulation and vascular biology.
  25. Adenosine Analog

    3’-O-Propargyladenosine is an adenosine analog that primarily targets adenosine receptors, acting as a vasodilator and exhibiting potential anti-cancer properties. It serves as a valuable tool in research applications involving click chemistry, due to its alkyne functional group, which facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This compound is instrumental in the study of biochemical pathways and therapeutic interventions related to adenosine signaling and vascular biology.
  26. Adenosine Analog

    N6-Bz-5'-O-DMTr-3'-deoxyadenosine-2'-O-CED-phosphoramidite is an adenosine analog that primarily targets adenosine receptors. It exhibits biological activities such as smooth muscle relaxation and has demonstrated potential in inhibiting cancer progression. This compound is useful in various research applications, particularly in the development of nucleic acid-based therapeutics and the study of adenosine receptor signaling pathways.
  27. Adenosine Analog

    5’-O-(4,4’-Dimethoxytrityl)-2’-beta-C-methyl adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound exhibits significant biological activities, including the inhibition of cancer progression. It serves as a valuable tool in research applications related to cardiovascular research, cancer therapies, and the study of adenosine receptor signaling pathways.
  28. Adenosine Analog

    N6-Benzoyl-2'-O-tert-butyldimethylsilyl-3'-O-DMT-adenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. This compound is valuable for research applications focusing on vascular biology, oncology, and the investigation of adenosine signaling pathways.
  29. Adenosine Analog

    N-[[4-(Trifluoromethyl)phenyl]methyl]adenosine is an adenosine analog known for its smooth muscle vasodilatory effects. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for research in oncology and cardiovascular studies. Its biological activity positions it as a key reagent for investigating adenosine receptor pathways and their implications in various therapeutic contexts.
  30. Adenosine Analog

    8-Benzyloxyadenosine is an adenosine analog that primarily targets adenosine receptors to elicit biological responses. This compound exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular biology and cancer therapeutics.
  31. Adenosine Analog

    5-Methyl-4’-thiouridine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects, promoting smooth muscle relaxation, and has shown potential in inhibiting cancer progression. Its applications in research encompass studies on cardiovascular function and cancer therapeutics.
  32. Adenosine Analog

    8-Bromo-5’-O-(4-cyanobenzyl)-2’,3’-di-O-isopropylidene adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory activity and has potential applications in cancer research due to its ability to inhibit cancer progression. Its structural modifications make it a valuable tool for studying adenosine signaling pathways in various biological systems.
  33. Adenosine Analog

    2'-O-t-Butyldimethylsilyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound functions as a smooth muscle vasodilator and has demonstrated potential in inhibiting cancer progression. It is valuable for research applications in vascular biology and oncology, contributing to studies on therapeutic pathways involving adenosine signaling.
  34. Adenosine Analog

    2-Benzylthioadenosine is an adenosine analog that primarily acts on adenosine receptors. It is known for its vasodilatory effects on smooth muscle and has been investigated for its potential to inhibit cancer progression. This compound is valuable in research applications related to cardiovascular health and oncology, contributing to the understanding of adenosine signaling pathways.
  35. Biochemical Assay Reagent

    Adenosine 2'-PEG-Biotin is a biochemical assay reagent that acts as a bioisostere of endogenous adenosine, allowing it to engage adenosine receptors effectively. This compound plays a crucial role in regulating various cell signaling pathways, facilitating research into its applications as a bioprobe, biosensor, or diagnostic reagent. Its incorporation of biotin also enhances its utility in various biochemical assays and detection methodologies.
  36. Adenosine Analog

    N6-Benzoyl-2',3'-isopropylidene adenosine is an adenosine analog targeting adenosine receptors. This compound exhibits significant smooth muscle vasodilatory activity and has demonstrated potential in inhibiting cancer progression. Its applications in research include studying vascular physiology and cancer biology, making it a valuable tool in the investigation of therapeutic strategies involving adenosine modulation.
  37. Adenosine Analog

    2'-O-Acetyl-3,5-bis-O-(2,4-dichlorobenzyl)adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory activity and has potential applications in inhibiting cancer progression. Its mechanism of action makes it a valuable tool for researchers studying cardiovascular function and cancer therapeutics.
  38. Adenosine Analog

    5′-O-[(4-Cyanophenyl)methyl]-2′,3′-O-(1-methylethylidene)adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits vasodilatory properties and demonstrates potential in inhibiting cancer cell proliferation. It is a valuable tool in research exploring the effects of adenosine signaling in cardiovascular diseases and cancer therapy.
  39. Adenosine Analog

    N4-Benzoyl-5'-O-DMT-2'-O-propargyl adenosine is an adenosine analog that acts primarily as a smooth muscle vasodilator. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for various biological research applications. Its distinctive structural properties facilitate the study of adenosine receptor interactions and signaling pathways, contributing to the understanding of cardiovascular physiology and tumor biology.
  40. Adenosine Analog

    N6-Benzyl-2’-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits vasodilatory effects in smooth muscle and demonstrates potential in inhibiting cancer progression. It serves as a valuable tool in studies focusing on cardiovascular function and cancer biology, facilitating research into therapeutic strategies for related conditions.
  41. Adenosine Analog

    N-[(3-Methoxyphenyl)methyl]adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant biological activity as a smooth muscle vasodilator and has demonstrated potential in inhibiting cancer progression. It is a valuable tool for researchers investigating vascular biology and cancer therapeutics.
  42. Uridine Analog

    5-Iodo-2’-β-C-methyl uridine is a uridine analog that primarily targets adenosine receptors. This compound exhibits potential antiepileptic properties and serves as a valuable tool in the investigation of anticonvulsant and anxiolytic activities. Additionally, it may contribute to the development of innovative antihypertensive agents in chemical research.
  43. Adenosine Analog

    5’-O-(4,4’-Dimethoxytrityl)-2’-O-(2-methoxyethyl) adenosine is an adenosine analog that primarily targets adenosine receptors. This compound demonstrates biological activities such as smooth muscle vasodilation and potential inhibition of cancer progression. It is valuable for research in cardiovascular studies and cancer biology, facilitating investigations into adenosine signaling and therapeutic applications.
  44. Adenosine Analog

    N6-Methyl-xylo-adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. Its unique properties make it a valuable tool for researchers investigating vascular biology and cancer therapies.
  45. 5'-AMP Analogue

    2-Cl-5'-AMP is a 5'-AMP analogue that functions primarily by interacting with adenosine receptors. This compound exhibits key biological activity in receptor mapping research, facilitating the study of adenosine receptor signaling pathways and their physiological roles. Its use in biochemical assays enables a deeper understanding of receptor-ligand interactions and their implications in various biological systems.
  46. Adenosine Analog

    N-Benzoyl-5'-O-dmtr-2'-O-(2-methoxyethyl)-adenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits significant vasodilatory effects by relaxing smooth muscle and has demonstrated potential in inhibiting cancer progression. This compound is valuable in biomedical research, particularly in studies focused on cardiovascular health and cancer therapy.
  47. Adenosine Analog

    9-(β-D-Xylofuranosyl)adenine is an adenosine analog that primarily acts as a vasodilator by targeting adenosine receptors. This compound has demonstrated significant biological activity, including the inhibition of cancer progression. It is particularly useful for researchers exploring the mechanisms of vasodilation and the therapeutic potential of adenosine-related pathways in cancer biology.
  48. Adenosine Analog

    2'-O-Methyladenosine 5'-monophosphate triethylammonium is an adenosine analog that primarily targets adenosine receptors. It exhibits significant biological activity, functioning as a smooth muscle vasodilator while also demonstrating potential for inhibiting cancer progression. This compound is valuable for research applications focusing on cardiovascular studies and cancer biology.
  49. Adenosine Analog

    8-Chloro-2'-deoxyadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant biological activity as a potential vasodilator and has demonstrated inhibitory effects on cancer progression. It is useful in various research applications, particularly in studying the pharmacological effects of adenosine and its derivatives in cardiovascular and oncology research.
  50. Adenosine Analog

    2-Methoxy-2'-deoxyadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits vasodilatory effects on smooth muscle and has demonstrated potential in inhibiting cancer progression, making it relevant for various research applications, including cardiovascular studies and oncology. Its structural similarity to adenosine allows for exploration in drug development targeting related pathways.

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