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8-Phenyltheophylline (8-Phenyl-1,3-dimethylxanthine, 8-PT) is a drug derived from the xanthine family which acts as a potent and selective antagonist for the adenosine receptors A1 and A2A, but unlike other xanthine derivatives has virtually no activity as a phosphodiesterase inhibitor. [1]

15 relations: Adenosine A1 receptor, Adenosine A2A receptor, Adenosine receptor, Binding selectivity, Caffeine, CYP1A2, Dipropylcyclopentylxanthine, Drug, Phosphodiesterase inhibitor, Potency (pharmacology), Receptor antagonist, Stimulant, Xanthine, 8-Chlorotheophylline, 8-Cyclopentyl-1,3-dimethylxanthine.

Adenosine A1 receptor

The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as endogenous ligand.

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Adenosine A2A receptor

The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it.

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Adenosine receptor

The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as endogenous ligand.

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Binding selectivity

Binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex.

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Caffeine is a central nervous system (CNS) stimulant of the methylxanthine class of psychoactive drugs.

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Cytochrome P450 1A2 (abbreviated CYP1A2), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body.

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8-Cyclopentyl-1,3-dipropylxanthine (DPCPX, PD-116,948) is a drug which acts as a potent and selective antagonist for the adenosine A1 receptor.

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A drug is, in the broadest of terms, a chemical substance that has known biological effects on humans or other animals.

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Phosphodiesterase inhibitor

A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s).

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Potency (pharmacology)

In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity.

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Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens agonist-mediated responses rather than provoking a biological response itself upon binding to a receptor.

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Stimulants (also referred to as psychostimulants) are psychoactive drugs that induce temporary improvements in either mental or physical functions or both.

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Xanthine (or; archaically xanthic acid) (3,7-dihydro-purine-2,6-dione), is a purine base found in most human body tissues and fluids and in other organisms.

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8-Chlorotheophylline, also known as 1,3-dimethyl-8-chloroxanthine, is a stimulant drug of the xanthine chemical class, with physiological effects similar to caffeine.

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8-Cyclopentyl-1,3-dimethylxanthine (8-Cyclopentyltheophylline, 8-CPT, CPX) is a drug which acts as a potent and selective antagonist for the adenosine receptors, with some selectivity for the A1 receptor subtype, as well as a non-selective phosphodiesterase inhibitor.

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[1] https://en.wikipedia.org/wiki/8-Phenyltheophylline

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