p1 receptor

RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC50 value of 2.5 μM and a Ymax of 65%. This compound exhibits significant microsomal stability, desirable pharmacokinetic properties, and pharmacodynamic activity. RXFP1 receptor agonist-9 is useful in the study of heart failure.

RXFP1 receptor agonist-10 (Compound 188) is an RXFP1 receptor agonist with an EC50 of 0.5 nM. It is useful for research into heart failure.

Example 2 (RXFP1 receptor agonist-8) is a potent RXFP1 receptor agonist that suppresses cAMP production in HEK293 cells expressing human RXFP1, exhibiting an EC50 of 1.8 nM [1].

RXFP1 receptor agonist-7 (Example 2) is an RXFP1 receptor agonist that effectively inhibits cAMP production in HEK293 cells stably expressing the human RXFP1, with an EC50 of 4.2 nM [1].

RXFP1 receptor agonist-6 (Example 7) acts as an agonist for the RXFP1 receptor and effectively suppresses cAMP production in HEK293 cells stably expressing the human RXFP1, with an EC50 of 12 nM [1].

RXFP1 receptor agonist-5 (Example 98) is an agonist targeting the RXFP1 receptor, inhibiting cAMP production in HEK293 cells with stable human RXFP1 expression, with an EC50 of 1.3 nM [1].

RXFP1 receptor agonist-4 (Example 268) is a potent RXFP1 receptor agonist, shown to effectively suppress cAMP production in HEK293 cells stably expressing the human RXFP1 receptor, with an effective concentration (EC50) of 4.9 nM [1].

RXFP1 receptor agonist-3 (Example 223) is an RXFP1 receptor agonist that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human RXFP1, with an EC50 of 2 nM [1].

RXFP1 Receptor Agonist-2 (Example 124), an EC50 value of 1 nM [1].

RXFP1 receptor agonist-1 (Example 2), suppresses cAMP production in HEK293 cells constitutively expressing the human RXFP1, with an EC50 of 300 nM [1].

Theophylline (1,3-Dimethylxanthine) is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac, and central nervous system stimulant activities. It inhibits the 3', 5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP, thus potentiating the actions of agents that act through adenylyl cyclases and cyclic AMP.

N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine) is an adenosine derivative and adenosine receptor agonist with Ki values of 11.8 nM for rat A1 receptors and 30.1 nM for human A1 receptors.

GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

MRS 1754 is a selective antagonist radioligand for the A2B adenosine receptor, exhibiting very low affinity for A1 and A3 receptors in both humans and rats.

A2A receptor antagonist 1 (CPI-444 analog) is an inhibitor of the adenosine A2A receptor and A1 receptor with Ki values of 4 nM and 264 nM, respectively.

Ticlopidine hydrochloride (Ticlodix) is an effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.

Inosine (NSC-20262), an endogenous purine nucleoside produced by the catabolism of adenosine, is an agonist of adenosine receptors A1R and A2AR. Inosine has anti-inflammatory, immunomodulatory, antinociceptive and neuroprotective effects.

Doxofylline (Doxophylline) is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has shown similar efficacy to theophylline but with significantly fewer side effects in animal and human studies.

Theobromine (3,7-Dimethylxanthine), a xanthine alkaloid, is used as a bronchodilator and as a vasodilator.

Adenosine 5'-monophosphate monohydrate (5'-AMP) , also known as 5'-adenylic acid, is a nucleotide that is used as a monomer in RNA. It is an ester of phosphoric acid and the nucleoside adenosine. Adenosine 5'-monophosphate monohydrate consists of a phosphate group, the sugar ribose, and the nucleobase adenine. As a substituent it takes the form of the prefix adenylyl-.

Diphylline (Diprophylline) is a xanthine derivative. Diphylline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Diphylline probably acts as a competitive inhibitor of phosphodiesterase which leads to an increase in intracellular cAMP. This results in relaxation of bronchial smooth muscle and other smooth muscles. Diphylline may also antagonize adenosinereceptors. Diphylline is used in the treatment of acute bronchial asthma, chronic bronchitis and emphysema.

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor giving a bronchodilatory effect.

Acefylline (Theophylline-7-acetic acid), a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects