A P2X PURINOCEPTOR CDNA CONFERRING A NOVEL PHARMACOLOGICAL PROFILE

被引:259
作者
BO, XN
ZHANG, Y
NASSAR, M
BURNSTOCK, G
SCHOEPFER, R
机构
[1] UNIV LONDON UNIV COLL, DEPT PHARMACOL, LONDON WC1E 6BT, ENGLAND
[2] UNIV LONDON UNIV COLL, WELLCOME LAB MOLEC PHARMACOL, LONDON WC1E 6BT, ENGLAND
[3] UNIV LONDON UNIV COLL, DEPT ANAT & DEV BIOL, LONDON WC1E 6BT, ENGLAND
基金
英国惠康基金;
关键词
PURINE RECEPTOR; P2-PURINOCEPTOR; ATP; SURAMIN; CNS;
D O I
10.1016/0014-5793(95)01203-Q
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We have cloned P2X(4), a member of the P2-purinoceptor family, which has a new pharmacological profile, Rat P2X(4) is distantly related to P2X(1), P2X(2) and P2X(3) 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 > ATP gamma S > 2-methylthio ATP > ADP approximate to alpha beta-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 P2X(4) it is unlikely that native P2X(4) has previously been recognized as a P2X purinoceptor.
引用
收藏
页码:129 / 133
页数:5
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