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1
The A3 adenosine receptor is the unique adenosine receptor which facilitates release of allergic mediators in mast cells.A3 腺苷受体是唯一能促进肥大细胞释放过敏介质的腺苷受体。
J Biol Chem. 1993 Aug 15;268(23):16887-90.
2
Riboflavin can protect tissue from oxidative injury.核黄素可以保护组织免受氧化损伤。
Nutr Rev. 1993 May;51(5):149-50. doi: 10.1111/j.1753-4887.1993.tb03092.x.
3
125I-4-aminobenzyl-5'-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A3 adenosine receptor.125I - 4 - 氨基苄基 - 5'-N - 甲基羧酰胺腺苷，一种对大鼠A3腺苷受体具有高亲和力的放射性配体。
Mol Pharmacol. 1994 May;45(5):978-82.
4
Adenosine A3 receptors in mast cells.肥大细胞中的腺苷A3受体
Trends Pharmacol Sci. 1994 Jan;15(1):13-4. doi: 10.1016/0165-6147(94)90124-4.
5
Functional characterization of the A2b adenosine receptor in NIH 3T3 fibroblasts.NIH 3T3成纤维细胞中A2b腺苷受体的功能特性
Biochem Pharmacol. 1994 Mar 2;47(5):801-14. doi: 10.1016/0006-2952(94)90480-4.
6
Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.N6-苄基腺苷-5'-脲酰胺作为A3选择性腺苷激动剂的构效关系
J Med Chem. 1994 Mar 4;37(5):636-46. doi: 10.1021/jm00031a014.
7
Effect of pertussis toxin treatment on the putative adenosine A3 receptor-mediated hypotensive response in the rat.百日咳毒素处理对大鼠假定的腺苷A3受体介导的降压反应的影响。
Eur J Pharmacol. 1993 Nov 30;250(1):185-8. doi: 10.1016/0014-2999(93)90641-t.
8
A binding site model and structure-activity relationships for the rat A3 adenosine receptor.大鼠A3腺苷受体的结合位点模型及构效关系
Mol Pharmacol. 1994 Jun;45(6):1101-11.
9
Selective ligands for rat A3 adenosine receptors: structure-activity relationships of 1,3-dialkylxanthine 7-riboside derivatives.大鼠A3腺苷受体的选择性配体：1,3 - 二烷基黄嘌呤7 - 核糖苷衍生物的构效关系
J Med Chem. 1994 Nov 11;37(23):4020-30. doi: 10.1021/jm00049a021.
10
Contrasting effects of adenosine A1 and A2 receptor ligands in different chemoconvulsive rodent models.腺苷A1和A2受体配体在不同化学惊厥啮齿动物模型中的对比作用
Eur J Pharmacol. 1993 Oct 5;242(3):221-8. doi: 10.1016/0014-2999(93)90245-d.

作为腺苷受体配体的非黄嘌呤衍生物的综述。

A SURVEY OF NONXANTHINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS.

作者信息

Siddiqi Suhaib M, Ji Xiao-Duo, Melman Neli, Olah Mark E, Jain Rahul, Evans Patricia, Glashofer Marc, Padgett William L, Cohen Louis A, Daly John W, Stiles Gary L, Jacobson Kenneth A

机构信息

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.

Departments of Medicine and Pharmacology, Duke University Medical Center, Durham, NC 27710.

出版信息

Nucleosides Nucleotides. 1996;15(1-3):693-717. doi: 10.1080/07328319608002416.

DOI:10.1080/07328319608002416
PMID:27043138
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4817726/
Abstract

The binding affinities at rat A, A, and A adenosine receptors of a wide range of heterocyclic derivatives have been determined. Mono-, bi-, tricyclic and macrocyclic compounds were screened in binding assays, using either [H]PIA or [H]CGS 21680 in rat brain membranes or [I]AB-MECA in CHO cells stably transfected with rat A receptors. Several new classes of adenosine antagonists ( 5-oxoimidazopyrimidines and a pyrazoloquinazoline) were identified. Various sulfonylpiperazines, 11-hydroxytetrahydrocarbazolenine, 4H-pyrido[1,2-a]pyrimidinone, folic acid, and cytochalasin H and J bound to A receptors selectively. Moreover, cytochalasin A, which bound to A adenosine receptors with K value of 1.9 μM, inhibited adenylyl cyclase in rat adipocytes, but not via reversible A receptor binding.

摘要

已测定了一系列杂环衍生物对大鼠A1、A2A和A2B腺苷受体的结合亲和力。在结合试验中，使用[3H]PIA或[3H]CGS 21680作用于大鼠脑膜，或使用[125I]AB-MECA作用于稳定转染大鼠A2A受体的CHO细胞，对单环、双环、三环和大环化合物进行了筛选。鉴定出了几类新的腺苷拮抗剂（5-氧代咪唑并嘧啶和吡唑并喹唑啉）。各种磺酰基哌嗪、11-羟基四氢咔唑啉、4H-吡啶并[1,2-a]嘧啶酮、叶酸以及细胞松弛素H和J选择性地与A2A受体结合。此外，细胞松弛素A以1.9 μM的K值与A1腺苷受体结合，可抑制大鼠脂肪细胞中的腺苷酸环化酶，但并非通过可逆性A1受体结合实现。