Jacobson K A, Trivedi B K, Churchill P C, Williams M
Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, Bethesda, MD 20892.
Biochem Pharmacol. 1991 May 15;41(10):1399-410. doi: 10.1016/0006-2952(91)90555-j.
A recent conference entitled held in Rockville, Maryland, in September, 1989, was one indication of the increasing interest in developing agonists and antagonists of P-(adenosine) and P-(ATP) purinoceptors [1] as potential therapeutic agents. Extracellular adenosine, acting at its membrane bound A and A receptors, is a ubiquitous modulator of cellular activity. The purine can arise from several sources including ATP hydrolysis by ectokinase activity in the region of the nerve terminal [2] and from -adenosylhomocysteine [3] and ATP within the cell. Together with its more stable analogs, adenosine is a potent inhibitor of neurotransmitter release in both the central and peripheral nervous systems, and in cardiac, adipose and other tissues. Adenosine can also affect blood pressure and heart rate as well as modulate the function of the immune, inflammatory, gastrointestinal, renal and pulmonary systems, either via its effects on transmitter release or directly via receptor mechanisms altering intracellular transduction processes.
1989年9月在马里兰州罗克维尔举行的一次名为 的近期会议，表明人们对开发P-（腺苷）和P-（ATP）嘌呤受体的激动剂和拮抗剂作为潜在治疗药物的兴趣日益浓厚[1]。细胞外腺苷作用于其膜结合的A和A受体，是细胞活性的一种普遍调节剂。嘌呤可来自多种来源，包括神经末梢区域外切激酶活性对ATP的水解[2]以及细胞内的 -腺苷同型半胱氨酸[3]和ATP。腺苷与其更稳定的类似物一起，是中枢和外周神经系统以及心脏、脂肪和其他组织中神经递质释放的有效抑制剂。腺苷还可影响血压和心率，并通过其对递质释放的影响或直接通过改变细胞内转导过程的受体机制来调节免疫、炎症、胃肠道、肾脏和肺部系统的功能。
