腺苷 5'-（β，γ-亚甲基）-二磷酸酯对映体与豚鼠膀胱的一些药理和生化相互作用。
Some pharmacological and biochemical interactions of the enantiomers of adenylyl 5'-(beta, gamma-methylene)-diphosphonate with the guinea-pig urinary bladder.
作者信息
Cusack N J, Hourani S M
出版信息
Br J Pharmacol. 1984 May;82(1):155-9. doi: 10.1111/j.1476-5381.1984.tb16453.x.
Abstract
Adenosine 5'-triphosphate (ATP) and adenylyl 5'-(beta, gamma-methylene)-diphosphonate (AMP-PCP) both contracted the guinea-pig urinary bladder, but the response to AMP-PCP was much greater. We synthesized the enantiomer of AMP-PCP, L-adenylyl 5'-(beta, gamma-methylene)-diphosphonate (L-AMP-PCP), and tested it on the guinea-pig bladder. L-AMP-PCP contracted the guinea-pig bladder, and was more potent than AMP-PCP and much more potent than ATP. The potential breakdown product of L-AMP-PCP, L-adenosine, unlike adenosine (the breakdown product of AMP-PCP), did not inhibit contractions of the guinea-pig bladder. ATP and its enantiomer L-adenosine 5'-triphosphate (L-ATP) were rapidly degraded by the muscle, and AMP-PCP was also degraded, but more slowly. L-AMP-PCP, however, was completely resistant to degradation. L-AMP-PCP would appear to be a useful ATP analogue, as it is potent and resistant to degradation, and its potential breakdown product, L-adenosine, is inactive.
摘要
腺苷5'-三磷酸（ATP）和腺苷5'-（β，γ-亚甲基）-二磷酸酯（AMP-PCP）均可使豚鼠膀胱收缩，但对AMP-PCP的反应要强得多。我们合成了AMP-PCP的对映体，即L-腺苷5'-（β，γ-亚甲基）-二磷酸酯（L-AMP-PCP），并在豚鼠膀胱上进行了测试。L-AMP-PCP可使豚鼠膀胱收缩，且比AMP-PCP更有效，比ATP更是强得多。L-AMP-PCP的潜在分解产物L-腺苷，与腺苷（AMP-PCP的分解产物）不同，它并不抑制豚鼠膀胱的收缩。ATP及其对映体L-腺苷5'-三磷酸（L-ATP）可被肌肉迅速降解，AMP-PCP也会被降解，但速度较慢。然而，L-AMP-PCP完全抗降解。L-AMP-PCP似乎是一种有用的ATP类似物，因为它效力强且抗降解，其潜在分解产物L-腺苷无活性。
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