Target intelligence / Profile preview

Purinergic P1 receptor

Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The purinergic P1 receptor, also known as the adenosine receptor, is a class of G protein-coupled receptors (GPCRs) that are activated by adenosine. These receptors play key roles in regulating physiological processes in various tissues throughout the body. There are four recognized subtypes: A1, A2A, A2B, and A3. Each subtype exhibits distinct tissue distribution and functional roles. They regulate diverse functions like neurotransmitter release, myocardial oxygen consumption, inflammatory responses, and immune system modulation. Drugs targeting these receptors have therapeutic applications, such as cardiac arrhythmia treatment, myocardial perfusion imaging, and the stimulant effects from dietary methylxanthines.

Other names
Adenosine receptor
02

Mechanism of action

A1 and A3: Coupled to Gi/Go proteins → inhibit adenylate cyclase → decrease cAMP levels. A2A and A2B: Coupled to Gs proteins → stimulate adenylate cyclase → increase cAMP levels

03

Biological functions

Neurotransmission modulationCardiovascular regulationImmune/inflammatory controlModulation of neurotransmitter releaseRegulation of myocardial oxygen consumption and coronary blood flowControl of inflammatory responsesImmune system modulation
04

Disease associations

Cardiac arrhythmiasInflammation
05

Interacting drugs

Adenosine

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