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Purinoceptors in the Nervous System *
Bertil B. Fredholm,
Bertil B. Fredholm
Department of Physiology and Pharmacology, Karolinska Institutet, S-171 77 Stockholm, Sweden
Search for more papers by this authorBertil B. Fredholm,
Bertil B. Fredholm
Department of Physiology and Pharmacology, Karolinska Institutet, S-171 77 Stockholm, Sweden
Search for more papers by this authorAuthor for correspondence: Bertil B. Fredholm, Department of Physiology and Pharmacology, Karolinska Institutet, S-171 77 Stockholm, Sweden (fax +46 8 33 16 53).
* This paper reflects the contents of a lecture presented at the XX IUPHAR Congress in Montreal, July 1994.
Abstract
Abstract: The purine nucleoside adenosine and the purine nucleotide ATP play different roles in the nervous system. Adenosine acts on a family of G protein coupled receptors, collectively called adenosine receptors or P1 purinoceptors. Four members of this family have been cloned and pharmacologically characterized: A1 A2a, A2b and A3. Their distribution, pharmacology and biological roles are briefly discussed. In particular, the evidence that adenosine acting at A1 receptors regulates the release of several neurotransmitters and that adenosine acting at A2a receptors modulates dopaminergic transmission is summarized. ATP acts on receptors called P2 purinoceptors, which appear to fall into at least two main families – G protein coupled receptors and intrinsic ion channels. Their subclassification is becoming clearer as receptors are cloned and new selective agonists and/or antagonists are becoming available. There is an interesting potential for development of drugs targeted at purines or their receptors.
Abbreviations
-
- ADP
-
- Adenosine diphosphate
-
- Ap4A
-
- Diadenosine tetraphosphate
-
- ATP
-
- Adenosine triphosphate
-
- BAPTA
-
- 1, 2-bis(2–aminophenoxy)ethane-N,N,N',N'-tetraacetic acid
-
- cAMP
-
- Cyclic adenosine 3′,5′-monophosphate
-
- CGS 21680
-
- 2-[p-(2-carbonylethyl)-phenylethylamino]-5′-N-ethylcarboxamidoadenosine
-
- DDT1MF-2
-
- (A smooth muscle cell line originally isolated from steroid-induced leiomyosarcoma of Syrian hamster vas deferens)
-
- DPCPX
-
- 1, 3-dipropyl-8-cyclopentylxanthine
-
- GABA
-
- γ-Aminobutyric acid
-
- IP3
-
- Inositol-(1,4,5)-triphosphate
-
- IUPHAR
-
- International Union of Pharmacology
-
- NMDA
-
- N-methyl-D-aspartate
-
- UTP
-
- Uridine triphosphate
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