GPR-137 Activators
GPR-137 can engage in diverse mechanisms to initiate the protein's signaling pathways. Forskolin, by directly stimulating adenylyl cyclase, produces an upsurge in cellular cAMP levels, a critical secondary messenger that activates protein kinase A (PKA). Once activated, PKA can phosphorylate various proteins, including GPR-137, thereby modulating its activity. Similarly, isoproterenol, a non-selective beta-adrenergic agonist, also enhances cAMP concentrations via the beta-adrenergic receptors, setting off a cascade that may culminate in the activation of GPR-137. Prostaglandin E2 (PGE2) and histamine operate through their respective G-protein-coupled receptors, with both agents increasing intracellular cAMP, enabling PKA to potentially modify GPR-137 activity through phosphorylation.
Adrenergic agents, dobutamine and epinephrine, through beta-1 and beta-adrenergic receptors respectively, escalate cAMP levels in certain tissues. Terbutaline and salbutamol, as beta-2 adrenergic receptor agonists, selectively prompt cAMP production in smooth muscle cells, which in turn activates PKA. If GPR-137 is present and responsive in these tissues, PKA could then phosphorylate the protein. Beta-Estradiol, which can activate G-protein-coupled receptors, may also lead to a rise in cAMP and subsequent PKA activation, influencing GPR-137 activity. Additionally, dopamine, through its neuronal G-protein-coupled receptors, and glucagon, by targeting its hepatic receptor, both result in increased cAMP, potentially facilitating GPR-137 phosphorylation via PKA. Lastly, adenosine's modulation of cAMP through its own set of receptors provides yet another avenue for the modulation of GPR-137 activity, assuming the protein is co-expressed and responsive to adenosine receptor activation.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Isoproterenol Hydrochloride | 51-30-9 | sc-202188 sc-202188A | 100 mg 500 mg | $28.00 $38.00 | 5 | |
Isoproterenol is a non-selective beta-adrenergic agonist, which can raise intracellular cAMP by activating adenylyl cyclase through the beta-adrenergic receptor. Elevated cAMP levels can lead to activation of protein kinase A (PKA), which may then phosphorylate and activate GPR-137 if GPR-137 is a substrate for PKA. | ||||||
PGE2 | 363-24-6 | sc-201225 sc-201225C sc-201225A sc-201225B | 1 mg 5 mg 10 mg 50 mg | $57.00 $159.00 $275.00 $678.00 | 37 | |
Prostaglandin E2 (PGE2) interacts with its G-protein-coupled receptors leading to increased intracellular cAMP levels, which can result in the activation of PKA. PKA might then target GPR-137 as part of a signaling cascade, leading to its activation. | ||||||
Histamine, free base | 51-45-6 | sc-204000 sc-204000A sc-204000B | 1 g 5 g 25 g | $94.00 $283.00 $988.00 | 7 | |
Histamine can bind to its G-protein-coupled histamine H2 receptor, increasing cAMP through adenylyl cyclase activation. Subsequently, PKA can be activated, which may phosphorylate GPR-137 leading to its activation. | ||||||
Dobutamine | 34368-04-2 | sc-507555 | 100 mg | $295.00 | ||
Dobutamine is a beta-1 adrenergic agonist that can increase cAMP levels in heart cells. If GPR-137 is expressed in cardiac tissue and is responsive to changes in cAMP, the action of dobutamine might activate GPR-137 through PKA signaling. | ||||||
(−)-Epinephrine | 51-43-4 | sc-205674 sc-205674A sc-205674B sc-205674C sc-205674D | 1 g 5 g 10 g 100 g 1 kg | $41.00 $104.00 $201.00 $1774.00 $16500.00 | ||
Epinephrine interacts with beta-adrenergic receptors, leading to an increase in cAMP and activation of PKA. PKA then potentially activates GPR-137 through phosphorylation if GPR-137 is present in the tissue and part of the adrenergic signaling pathway. | ||||||
Terbutaline Hemisulfate | 23031-32-5 | sc-204911 sc-204911A | 1 g 5 g | $92.00 $378.00 | 2 | |
Terbutaline, a beta-2 adrenergic agonist, can elevate cAMP levels, leading to PKA activation. PKA, in turn, may activate GPR-137 by phosphorylating it if GPR-137 is part of the beta-adrenergic response pathway in cells. | ||||||
Salbutamol | 18559-94-9 | sc-253527 sc-253527A | 25 mg 50 mg | $94.00 $141.00 | ||
Salbutamol is a selective beta-2 adrenergic receptor agonist increasing intracellular cAMP levels. This rise in cAMP can lead to the activation of PKA, which could potentially phosphorylate and activate GPR-137 if the protein is involved in this pathway. | ||||||
β-Estradiol | 50-28-2 | sc-204431 sc-204431A | 500 mg 5 g | $63.00 $182.00 | 8 | |
Beta-Estradiol has been shown to activate certain GPRs through non-genomic pathways. If GPR-137 is similarly affected, Beta-Estradiol may lead to activation through secondary messenger systems such as cAMP. | ||||||
Dopamine | 51-61-6 | sc-507336 | 1 g | $290.00 | ||
Dopamine can function through its G-protein-coupled receptors to increase cAMP levels in certain neuronal pathways. While GPR-137's role in dopaminergic signaling is not well-established, dopamine may activate GPR-137 through cAMP-dependent PKA phosphorylation in those pathways. | ||||||
Adenosine | 58-61-7 | sc-291838 sc-291838A sc-291838B sc-291838C sc-291838D sc-291838E sc-291838F | 1 g 5 g 100 g 250 g 1 kg 5 kg 10 kg | $34.00 $48.00 $300.00 $572.00 $1040.00 $2601.00 $4682.00 | 1 | |
Adenosine interacts with its G-protein-coupled receptors to modulate cAMP levels. Depending on the cell type and the expression of GPR-137, the adenosine-induced changes in cAMP could lead to the activation of GPR-137 through PKA-mediated phosphorylation. | ||||||