A P2X purinoceptor cDNA conferring a novel pharmacological profile

FEBS Letters

Burnstock, Geoffrey²  Bo, Xuenong²  Nassar, Mohammed¹  Schoepfer, Ralf¹  Zhang, Yi² 

[1] Wellcome Laboratory for Molecular Pharmacology and Department of Pharmacology, University College London, Gower Street, London WC 1E 6BT, UK;Department of Anatomy and Developmental Biology, University College London, Gower Street, London, WC 1E 6BT, UK

关键词: Purine receptor;    P2-purinoceptor;    ATP;    Suramin;    CNS;   

DOI  :  10.1016/0014-5793(95)01203-Q

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

We have cloned P2X₄, a member of the P2-purinoceptor family, which has a new pharmacological profile. Rat P2X₄ is distantly related to P2X₁, P2X₂ and P2X₃ and is expressed in brain, spinal cord, lung, thymus, bladder, adrenal, testis and vas deferens. This ligand gated ion channel is activated by ATP and analogs with the potency order of ATP > ATPγS > 2-methylthio ATP > ADP ≈ αβ-methylene ATP. However, none of the currently used P2X purinoceptor antagonists suramin, reactive blue 2 and PPADS blocked ATP evoked currents; in contrast their application resulted in potentiation of the agonist response. Due to lack of any known antagonist for P2X₄ it is unlikely that native P2X₄ has previously been recognized as a P2X purinoceptor.

【 授权许可】

Unknown