camp accumulation

Ro 67-7476 is a positive allosteric modulator of mGluR1, which can enhance the calcium release induced by glutamate in HEK293 cells expressing rat mGluR1a. The EC50 is 60.1 nM. It is a P-ERK1/2 agonist, and can activate ERK1/2 phosphorylation without the addition of exogenous glutamate (EC50 = 163.3 nM).

Telcagepant (MK-0974) is an oral calcitonin gene-related peptide receptor (CGRP) antagonist that blocks CGRP receptors and reduces neurotransmission in the central nervous system and is used in the study of migraines and for pain relief.

Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM. Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM.

3-Methylvaleric Acid is an edible grade flavor present in tobacco.3-Methylvaleric Acid enhances intracellular cAMP accumulation and CRE-luciferase activity in CHO-K1 cells and HEK293 cells.

Apelin-17 (human, bovine) acetate is an endogenous apelin receptor agonist. Potently inhibits forskolin-stimulated cAMP accumulation (pIC50 = 9.94).

Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist that promotes cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR (EC50: 22 nM). It is used to treat overactive bladder and irritable bowel syndrome.

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

DD202-114 is an effective and selective agonist of GLP1R. It promotes the accumulation of cAMP, reduces blood glucose levels, and decreases food intake. Additionally, DD202-114 holds potential for research in type 2 diabetes mellitus (T2DM) and obesity studies.

ECC5004 is a compound that activates the glucagon-like peptide-1 receptor (GLP-1R). In HEK293 cells expressing the human GLP-1R, ECC5004 induces cAMP accumulation with an EC50 value of less than 20 nM.

Trequinsin HCl is a phosphodiesterase (PDE) 3 inhibitor dependent on cyclic adenosine monophosphate (cAMP). It facilitates the accumulation of cAMP and enhances cell membrane capacitance.

GLP-1R agonist 27 (compound 21) is a potent and orally active GLP-1R agonist. It enhances the accumulation of cyclic adenosine monophosphate (cAMP), reduces blood glucose levels, and decreases food intake. GLP-1R agonist 27 shows potential for research in obesity and type 2 diabetes mellitus (T2DM).

FFA2 agonist-1 (Compound 4) is an agonist of the free fatty acid receptor 2 (FFA2/GPR43) with an EC50 of 81 nM. It demonstrates activity in β-arrestin-2 recruitment and cAMP inhibition assays, with EC50 values of 1.2 μM and 0.53 μM, respectively. FFA2 agonist-1 can induce the mucosal response of appetite-regulating peptide YY (PYY), inhibit fat accumulation, and affect intestinal function and food intake, making it useful for obesity research.

ZP3022 is a dual agonist targeting the glucagon-like peptide 1 receptor (GLP-1R) and cholecystokinin 2 (CCK2) receptor. It selectively enhances cAMP accumulation or ERK phosphorylation in HEK293 cells with GLP-1R or CCK2 receptor expression, compared to ERK phosphorylation in cells with the CCK1 receptor (EC50s: 0.02, 10.3, and >1,000 nM for human receptors, respectively). At 40 nM, ZP3022 promotes proliferation of rat neonatal β-cells in vitro. It also boosts glucose-induced insulin secretion (GSIS) in rat pancreatic islets at 10 and 100 nM concentrations and decreases body weight in rats at 40 nmol/kg doses twice daily. Administered at 100 nmol/kg daily, ZP3022 enhances β-cell and total pancreatic mass and improves glucose tolerance in db/db mice, while reducing food intake but not body weight in these mice.

TGR5 agonist 5 (compound K91) is an effective activator of TGR5, with an EC50 of 19 μM in the CRE-Luciferase assay and 30 μM in the cAMP accumulation assay.

Adenosine receptor agonist2 (Compound 10) is an agonist of the adenosine A2B receptor (A2BR) with an EC50 of 0.38 nM. It significantly inhibits the accumulation of cAMP and calcium ions. Adenosine receptor agonist2 is applicable in cardiovascular protection studies.

Raxlaprazine etomoxil is a modulator of dopamine D2 and D3 receptors, applicable in psychiatric disorder research. It exhibits a Ki of 1.95 nM for human recombinant D2L receptors and an EC50 of 3.72 nM for forskolin-stimulated cAMP accumulation.

ST171 is a dual-action 5-HT1AR agonist with a Ki of 0.41 nM. It selectively activates the Gi/o signaling pathway and inhibits cAMP accumulation mediated by 5-HT1AR, without Gs activation and with minimal β-arrestin recruitment. ST171 reduces hypersensitivity in mouse models of chronic neuropathic and inflammatory pain and is applicable for pain research.

KOR agonist 6 is a KOR agonist with a Ki value of 0.25 pM. In CHO cells, it exhibits agonistic activity on MOR and DOR and inhibits forskolin-stimulated cAMP accumulation. The compound stimulates KOR-mediated [35S]GTPγS binding in HEK293 cells expressing KOR and effectively suppresses cAMP accumulation as a potent agonist, showing lower β-arrestin recruitment efficacy. Additionally, KOR agonist 6 demonstrates analgesic effects in mice and can be employed in the study of analgesics with reduced central nervous system (CNS) side effects.

AM12814 is a potent partial agonist for the CB1 and CB2 receptors, with Ki values of 0.7 nM and 3.4 nM, respectively. It inhibits cAMP accumulation and recruits β-arrestin 2. AM12814 exhibits cannabinoid-like effects and can be used in research on neurological disorders, such as catalepsy.

MRS8454 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR). It significantly enhances the maximal effect of the standard agonist Cl-IB-MECA to approximately 286%-300% and notably decreases its EC50 value. MRS8454 effectively augments the ability of A3AR agonists to inhibit forskolin-induced cAMP accumulation and can be utilized in the development of molecular probes.

XYDC2050 (Compound 29) is a selective vasopressin V2 receptor (V2R) antagonist, with an IC50 of 27 nM and a Ki of 2.8 nM. It exhibits a Ki of 420.7 nM for V1R with a selectivity index of 162. XYDC2050 inhibits vasopressin-induced intracellular cyclic adenosine monophosphate (cAMP) accumulation with an IC50 of 12 nM. This compound can suppress kidney cyst growth, reduce kidney-to-body weight ratio, and decrease cyst area and cystic index, making it a candidate for autosomal dominant polycystic kidney disease (ADPKD) research.

TGR5 agonist 9 is a highly selective, orally active allosteric agonist of TGR5, exhibiting EC₅₀ values of 0.48 μM for hTGR5 and 0.49 μM for mTGR5. It recruits β-arrestin 1 (EC₅₀= 78.8 μM) and β-arrestin 2 (EC₅₀= 12.3 μM), and demonstrates enhanced efficacy in cAMP accumulation (EC₅₀= 0.48 μM). In ICR mouse models, TGR5 agonist 9 shows significant hypoglycemic effects, making it a potential candidate for diabetes research.

GLP-1R agonist 40 (Compound I-1) is an orally active and potent selective GLP-1R agonist with an EC50 of 26.7 pM for cAMP accumulation. It significantly reduces blood glucose levels and can be utilized in research related to type 2 diabetes.

RS 23597-190 hydrochloride is an indole derivative and a potent, selective 5-HT4 receptor antagonist (pKi = 9.1). It acts by blocking 5-HT4-mediated cAMP accumulation with high selectivity, used for gastrointestinal motility and arrhythmia research.