Lukacsko P, Krell R D
Eur J Pharmacol. 1982 Jun 4;80(4):401-6. doi: 10.1016/0014-2999(82)90086-3.
The ability of purines and pyrimidines to cause and inhibit contractile responses was examined in strips of guinea-pig urinary bladder. Adenosine 5'-triphosphate (ATP), beta, gamma-methylene ATP (APPCP), adenosine 5'-diphosphate (ADP), guanosine 5'-triphosphate (GTP) and cytidine 5'-triphosphate (CTP) caused concentration-dependent contractions of the bladder. The order of potency was APPCP greater than ATP greater than GTP=CTP greater than ADP. Adenosine 5'-monophosphate, adenosine, guanosine 5'-diphosphate, guanosine 5'-monophosphate, guanosine, cytidine 5'-diphosphate, cytidine 5'-monophosphate, adenosine, guanosine 5'-diphosphate, guanosine 5'-monophosphate, guanosine, cytidine 5'-diphosphate, cytidine 5'-monophosphate and cytidine had no apparent contractile activity up to 10(-3) M. Cumulative administrations of 5 X 10(-4) M APPCP, ATP, ADP, GTP or CTP resulted in complex desensitization of the tissue to the contractile activity of the nucleotide. Tissues desensitized to GTP or CTP were non-responsive to ATP suggesting cross-tachyphylaxis. Nucleotides lacking contractile activity or nucleosides did not alter the response of the bladder to ATP; except AMP and adenosine which significantly reduced the contraction. These results suggest that the polyphosphate structure, and not the base, is the determining portion of the nucleotide for promoting contractile activity and the development of tachyphylaxis.
在豚鼠膀胱条上研究了嘌呤和嘧啶引起及抑制收缩反应的能力。三磷酸腺苷（ATP）、β，γ-亚甲基三磷酸腺苷（APPCP）、二磷酸腺苷（ADP）、三磷酸鸟苷（GTP）和三磷酸胞苷（CTP）可引起膀胱的浓度依赖性收缩。效力顺序为APPCP＞ATP＞GTP = CTP＞ADP。一磷酸腺苷、腺苷、二磷酸鸟苷、一磷酸鸟苷、鸟苷、二磷酸胞苷、一磷酸胞苷、腺苷、二磷酸鸟苷、一磷酸鸟苷、鸟苷、二磷酸胞苷、一磷酸胞苷和胞苷在浓度高达10⁻³ M时无明显收缩活性。累积给予5×10⁻⁴ M的APPCP、ATP、ADP、GTP或CTP会导致组织对核苷酸收缩活性产生复杂的脱敏作用。对GTP或CTP脱敏的组织对ATP无反应，提示交叉快速耐受性。缺乏收缩活性的核苷酸或核苷不会改变膀胱对ATP的反应；但一磷酸腺苷和腺苷会显著减弱收缩。这些结果表明，多磷酸结构而非碱基是核苷酸促进收缩活性和产生快速耐受性的决定性部分。
