OR4A16 Activators
Chemical activators of OR4A16 can influence its function through various intracellular signaling pathways that ultimately lead to the protein's activation. Isoproterenol, Forskolin, IBMX, Epinephrine, Dopamine, Histamine, Adenosine, PGE2, Salmeterol, and Terbutaline all engage in processes that converge on the elevation of cyclic adenosine monophosphate (cAMP) within olfactory sensory neurons. Isoproterenol, a beta-adrenergic agonist, stimulates the adenylyl cyclase pathway, thereby increasing cAMP levels, which in turn activates protein kinase A (PKA). This activation can lead to the phosphorylation of OR4A16, enhancing its sensitivity. Forskolin directly stimulates adenylyl cyclase, bypassing receptor activation to increase cAMP and stimulate PKA, which then may activate OR4A16. IBMX functions by inhibiting the breakdown of cAMP, sustaining its elevated levels and facilitating the continued activation of PKA and subsequent phosphorylation of OR4A16.
Epinephrine, Dopamine, and Histamine exert their effects by binding to their respective G protein-coupled receptors, which indirectly lead to the activation of adenylyl cyclase and an increase in cAMP production. The resultant PKA activation can lead to the phosphorylation of OR4A16. Adenosine, through its action on A2A receptors, and PGE2, through EP2 and EP4 receptors, also promote the formation of cAMP and subsequent PKA activation, suggesting a similar mechanism of OR4A16 activation. Salmeterol and Terbutaline, both beta2-adrenergic receptor agonists, stimulate adenylyl cyclase activity to increase cAMP levels, which in turn activates PKA and may lead to OR4A16 phosphorylation and activation. Vardenafil and Rolipram, although they target the phosphodiesterase enzymes that break down cyclic guanosine monophosphate (cGMP) and cAMP respectively, also contribute to the activation of PKA due to the resulting increase in cyclic nucleotide levels, which can have a broad impact on sensory signal transduction, including the activation of OR4A16.
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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 | $27.00 $37.00 | 5 | |
Isoproterenol, a beta-adrenergic agonist, leads to the activation of the adenylyl cyclase pathway, which in turn increases cAMP levels within the cell. Elevated cAMP can activate PKA, which may lead to phosphorylation and activation of proteins, including olfactory receptors like OR4A16, thereby enhancing their sensitivity to olfactory ligands. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin directly stimulates adenylyl cyclase, increasing intracellular cAMP levels. This rise in cAMP activates PKA, which can then phosphorylate and activate OR4A16, as phosphorylation is a common regulatory mechanism for olfactory receptors. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $159.00 $315.00 $598.00 | 34 | |
3-Isobutyl-1-methylxanthine (IBMX) is a non-specific inhibitor of phosphodiesterases, which prevents the breakdown of cAMP and cGMP, leading to their accumulation. The increased cAMP levels can activate PKA, potentially resulting in the phosphorylation and functional activation of OR4A16. | ||||||
(−)-Epinephrine | 51-43-4 | sc-205674 sc-205674A sc-205674B sc-205674C sc-205674D | 1 g 5 g 10 g 100 g 1 kg | $40.00 $102.00 $197.00 $1739.00 $16325.00 | ||
Epinephrine interacts with adrenergic receptors, which can indirectly lead to the activation of adenylyl cyclase and an increase in cAMP production. This cascade activates PKA, which could phosphorylate and activate OR4A16 as part of the signal transduction in olfactory neurons. | ||||||
Dopamine | 51-61-6 | sc-507336 | 1 g | $290.00 | ||
Dopamine binds to its G protein-coupled receptors, which can activate adenylyl cyclase in certain pathways, raising cAMP levels. The subsequent activation of PKA may lead to phosphorylation and functional activation of OR4A16 in olfactory sensory neurons. | ||||||
Histamine, free base | 51-45-6 | sc-204000 sc-204000A sc-204000B | 1 g 5 g 25 g | $92.00 $277.00 $969.00 | 7 | |
Histamine can bind to H2 receptors, which are coupled to Gs proteins, leading to the activation of adenylyl cyclase and an increase in cAMP. The elevated cAMP activates PKA, which might phosphorylate and activate OR4A16 in olfactory sensory 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 | $33.00 $47.00 $294.00 $561.00 $1020.00 $2550.00 $4590.00 | 1 | |
Adenosine interacts with A2A receptors, a subset of which can activate adenylyl cyclase via Gs proteins, leading to elevated cAMP levels and PKA activation. PKA could subsequently phosphorylate and activate OR4A16 within olfactory signal transduction pathways. | ||||||
PGE2 | 363-24-6 | sc-201225 sc-201225C sc-201225A sc-201225B | 1 mg 5 mg 10 mg 50 mg | $56.00 $156.00 $270.00 $665.00 | 37 | |
Prostaglandin E2 (PGE2) binds to EP2 and EP4 receptors, which are coupled to Gs proteins that stimulate adenylyl cyclase, raising cAMP levels. The activation of PKA may then phosphorylate and activate OR4A16, as part of the olfactory transduction process. | ||||||
Vardenafil | 224785-90-4 | sc-362054 sc-362054A sc-362054B | 100 mg 1 g 50 g | $516.00 $720.00 $16326.00 | 7 | |
Vardenafil is a phosphodiesterase type 5 inhibitor, leading to the prevention of cGMP breakdown, which can have a broad impact on sensory signal transduction. Although less direct, increased cGMP may enhance cAMP signaling, potentially resulting in PKA activation and subsequent phosphorylation and activation of OR4A16. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $75.00 $212.00 | 18 | |
Rolipram is a selective inhibitor of phosphodiesterase 4, which degrades cAMP. Inhibition by Rolipram results in elevated cAMP levels, which can activate PKA. PKA, in turn, may phosphorylate and activate OR4A16 in olfactory sensory neurons. | ||||||