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P1- and P2-purinoceptor subtypes--an update.
1Department of Pharmacology, University of Cambridge, U.K.
Archives Internationales De Pharmacodynamie Et De Therapie
|January 1, 1990
Summary
Purinergic receptors are not uniform; P1 receptors include A1 and A2 subtypes, with evidence for A3. P2 receptors can be divided into P2x and P2y subtypes, each with specific agonists and antagonists.
Area of Science:
- Pharmacology
- Biochemistry
- Molecular Biology
Background:
- Purinergic receptors, involved in cellular signaling, were initially considered homogeneous groups.
- Recent research suggests heterogeneity within P1 and P2 purinergic receptor families.
Purpose of the Study:
- To investigate the subtypes of P1 and P2 purinergic receptors.
- To differentiate receptor subtypes based on biochemical, ligand binding, and pharmacological data.
Main Methods:
- Utilizing biochemical assays to analyze receptor composition.
- Employing ligand binding studies to determine receptor affinity.
- Conducting pharmacological experiments with specific agonists and antagonists.
Main Results:
- P1 purinoceptors are subdivided into A1 and A2 subtypes, with supporting evidence for A3.
- P2 purinoceptors are divided into P2x and P2y subtypes based on agonist potency and antagonist activity.
- Specific agonists like beta,gamma-methylene-L-ATP (P2x) and ADP-beta-F (P2y) were identified.
- Suramin antagonizes both P2x and P2y, while reactive blue 2 shows selectivity for P2y.
Conclusions:
- P1 and P2 purinergic receptors represent heterogeneous receptor families.
- The A1, A2, and potentially A3 subtypes constitute the P1 purinoceptor group.
- The P2 purinoceptor family includes P2x and P2y subtypes, with emerging evidence for P2t and P2z receptors.