## Abstract The increasing number of ATPβ and UTPβsensitive membrane receptors identified by cloning represent either ligandβactivated ion channels (P2X) or Gβproteinβcoupled receptors (P2Y). Adenosine, ATP, and UTP have potential application in the management of pain, cancer, and some cardiovascul
Avian and human homologues of the P2Y1 receptor: Pharmacological, signaling, and molecular properties
β Scribed by Jose L. Boyer; Joel B. Schachter; Susan M. Sromek; R. Kyle Palmer; Kenneth A. Jacobson; Robert A. Nicholas; T. Kendall Harden
- Publisher
- John Wiley and Sons
- Year
- 1996
- Tongue
- English
- Weight
- 835 KB
- Volume
- 39
- Category
- Article
- ISSN
- 0272-4391
No coin nor oath required. For personal study only.
β¦ Synopsis
The P2Y receptor on turkey erythrocyte membranes was the first P2 receptor to be shown to activate phospholipase C (PLC) in a strictly guanine nucleotide-dependent manner and remains the only G protein-coupled P2 receptor for which G protein-coupling kinetics have been defined. This membrane receptor has provided a model system for detailed pharmacological analyses of a series of chain-extended 2-thioether derivatives of adenine nucleotides that exhibit remarkable selectivity and potency for P2Y receptors. This model system also has led recently to identification of a novel series of P2 receptor antagonists. The turkey erythrocyte receptor is the species homologue of the chick P2Y1 receptor originally cloned by Webb and coworkers [Webb et al., 19931. We also have cloned the human homologue of the P2Y1 receptor, which exhibits identical pharmacological and second messenger signaling properties to that of the avian P2Y1 receptor.
π SIMILAR VOLUMES
The biological actions of extracellular nucleotides are exerted via two families of P2 receptors, P2X and P2Y. The metabotropic P2Y receptors comprise at least 7 distinct subtypes, which have been cloned from a number of species. However, none of the P2Y receptor proteins have been visualised yet in