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P2Y Receptors: Focus on Structural, Pharmacological and Functional Aspects in the Brain

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Abstract:

Purine and pyrimidine nucleotides have been identified as potent extracellular signalling molecules, acting at two classes of cell surface receptors, ionotropic P2X and metabotropic P2Y receptor (-R) types. Hitherto eight subtypes of the P2Y-R family have been cloned from mammalian species that exhibit sensitivity to the adenine nucleotides ATP/ADP (P2Y1,11,12,13), the uracil nucleotides UTP/UDP (P2Y2,4,6 or UDP-glucose in the case of P2Y14) or both adenine and uracil nucleotides (P2Y2). The P2Y-Rs are G proteincoupled receptors activating phospholipase C via Gαq/11 protein and stimulating or inhibiting adenylyl cyclase via Gαs and Gαi/o proteins, respectively. These receptors may activate distinct signalling cascades. Although classical models predict that P2Y-Rs exist in the cell membrane as monomers, homo- or heterodimeric assemblies may be generated. Interactions with certain ion channels or ligand-gated receptors as well as the co-localization of several receptor subtypes in the same cell provide the basis for a high functional diversity. The proteins for various P2Y-Rs are expressed early in the embryonic brain and are broadly distributed on both, neurons and astroglial cells. P2Y-R involvement in the regulation of normal physiological processes on the cellular level or in vivo, such as modulation of transmitter release, generation of astroglial Ca2+ waves, in diverse effects on behavioural functions and in the etiopathology of neurodegenerative diseases, are discussed and own data are presented. However, the exact understanding of the role of individual P2Y-R subtypes is still limited. Concerning the potentially important functions of P2Y-Rs, there is a strong need to develop stable, lipophilic and subtypeselective P2Y-R ligands, which may open new therapeutic strategies.

Keywords: ATP; Astrocytes; behaviour; neurodegenerative diseases; neurons; purinergic signalling; synaptic transmission

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986707782023695

Affiliations: Rudolf-Boehm-Institute of Pharmacology and Toxicology, University of Leipzig, Haertelstrasse 16-18, D-04107 Leipzig,Germany.

Publication date: October 1, 2007

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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