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苯乙醇胺N-甲基转移酶抑制剂对肾上腺肾上腺素生物合成的长期影响。

The long term effects of an inhibitor of phenylethanolamine N-methyltransferase upon adrenal epinephrine biosynthesis.

作者信息

Pendleton R G, Gessner G, Jenkins B

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1976 Nov;295(2):127-33. doi: 10.1007/BF00499444.

DOI:10.1007/BF00499444
PMID:825786
Abstract

Chronic administration of SK&F 64139, an inhibitor of phenylethanolamine N-methyltransferase (PNMT), initially resulted in a lowered adrenal epinephrine content in both the rat and squirrel monkey adrenal gland. With continued dosing, however, these levels returned toward control. The latter changes were accompanied by increased adrenal levels of norepinephrine and PNMT, but not by decreased plasma drug levels. These results suggest that long-term pharmacological PNMT inhibition may evoke compensatory mechanisms to maintain adrenal epinephrine biosynthesis under basal laboratory conditions.

摘要

长期给予苯乙醇胺N-甲基转移酶(PNMT)抑制剂SK&F 64139,最初会导致大鼠和松鼠猴肾上腺中肾上腺素含量降低。然而,持续给药后,这些水平又恢复到对照水平。后一种变化伴随着肾上腺中去甲肾上腺素和PNMT水平的升高,但血浆药物水平并未降低。这些结果表明,在基础实验室条件下,长期药理抑制PNMT可能会引发代偿机制以维持肾上腺肾上腺素的生物合成。

相似文献

1
The long term effects of an inhibitor of phenylethanolamine N-methyltransferase upon adrenal epinephrine biosynthesis.苯乙醇胺N-甲基转移酶抑制剂对肾上腺肾上腺素生物合成的长期影响。
Naunyn Schmiedebergs Arch Pharmacol. 1976 Nov;295(2):127-33. doi: 10.1007/BF00499444.
2
Studies on adrenal phenylethanolamine N- methyltransferase (PNMT) with S K & F 64139, a selective inhibitor.用选择性抑制剂S K & F 64139对肾上腺苯乙醇胺N-甲基转移酶(PNMT)进行的研究。
J Pharmacol Exp Ther. 1976 Jun;197(3):623-32.
3
Studies on SK&F 29661, an organ-specific inhibitor of phenylethanolamine N-methyltransferase.对苯乙醇胺N-甲基转移酶的器官特异性抑制剂SK&F 29661的研究。
J Pharmacol Exp Ther. 1979 Jan;208(1):24-30.
4
The effect of phenylethanolamine n-methyltransferase concentration and species difference on the inhibitory potency of SK&F 64139.苯乙醇胺N-甲基转移酶浓度和物种差异对SK&F 64139抑制效力的影响。
Res Commun Chem Pathol Pharmacol. 1977 Jun;17(2):201-13.
5
Studies on the long term effects of SK&F 29661 upon adrenal catecholamines.关于SK&F 29661对肾上腺儿茶酚胺长期影响的研究。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Apr;319(1):22-8. doi: 10.1007/BF00491473.
6
The effects of an inhibitor of phenylethanolamine N-methyltransferase upon stimulated adrenal catecholamine release and excretion in the rat.苯乙醇胺N-甲基转移酶抑制剂对大鼠肾上腺儿茶酚胺释放及排泄的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1977 Apr;297(3):245-50. doi: 10.1007/BF00509268.
7
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 1. Chloro-substituted 1,2,3,4-tetrahydroisoquinolines.苯乙醇胺N-甲基转移酶和肾上腺素生物合成的抑制剂。1. 氯取代的1,2,3,4-四氢异喹啉。
J Med Chem. 1980 May;23(5):506-11. doi: 10.1021/jm00179a007.
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Possible mechanism of action of SKF 64139 in vivo on rat adrenal and brain phenylethanolamine N-methyltransferase activity.SKF 64139对大鼠肾上腺和脑苯乙醇胺N-甲基转移酶活性的体内作用可能机制。
Biochem Pharmacol. 1988 Jan 15;37(2):313-8. doi: 10.1016/0006-2952(88)90734-4.
9
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 2. 1,2,3,4-Tetrahydroisoquinoline-7-sulfonanilides.苯乙醇胺N-甲基转移酶和肾上腺素生物合成的抑制剂。2. 1,2,3,4-四氢异喹啉-7-磺酰苯胺类化合物。
J Med Chem. 1980 Aug;23(8):837-40. doi: 10.1021/jm00182a005.
10
Epinephrine synthesis in the rat iris.大鼠虹膜中的肾上腺素合成
Invest Ophthalmol Vis Sci. 1990 Apr;31(4):677-80.

引用本文的文献

1
Studies on the long term effects of SK&F 29661 upon adrenal catecholamines.关于SK&F 29661对肾上腺儿茶酚胺长期影响的研究。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Apr;319(1):22-8. doi: 10.1007/BF00491473.
2
The effects of an inhibitor of phenylethanolamine N-methyltransferase upon stimulated adrenal catecholamine release and excretion in the rat.苯乙醇胺N-甲基转移酶抑制剂对大鼠肾上腺儿茶酚胺释放及排泄的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1977 Apr;297(3):245-50. doi: 10.1007/BF00509268.

本文引用的文献

1
Catecholamine production and release in exposure and acclimation to cold.暴露于寒冷及适应寒冷过程中儿茶酚胺的产生与释放
Acta Physiol Scand Suppl. 1961;183:1-101.
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Catecholamine excretion following carbon tetrachloride administration.四氯化碳给药后的儿茶酚胺排泄情况。
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Purification and properties of phenylethanolamine-N-methyl transferase.苯乙醇胺-N-甲基转移酶的纯化及性质
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Adaptive increases in drug-metabolizing enzymes induced by phenobarbital and other drugs.苯巴比妥及其他药物诱导的药物代谢酶适应性增加。
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Observations on the drug-induced synthesis of D-glucuronic, L-gulonic and L-ascorbic acids in rats.关于药物诱导大鼠体内D-葡萄糖醛酸、L-古洛糖酸和L-抗坏血酸合成的观察
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Fluorometric measurement of rat plasma and adrenal corticosterone concentration; a note on technical details.大鼠血浆和肾上腺皮质酮浓度的荧光测定;技术细节说明
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J Biol Chem. 1957 Aug;227(2):785-94.
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A simple ultraviolet spectrophotometric method for the determination of protein.一种测定蛋白质的简易紫外分光光度法。
J Lab Clin Med. 1956 Aug;48(2):311-4.
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A rapid, simple method for the determination of reduced, dehydro-, and total ascorbic acid in biological material.一种用于测定生物材料中还原型、脱氢型和总抗坏血酸的快速、简便方法。
J Biol Chem. 1955 Jan;212(1):59-68.
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Distribution of adrenaline and nonadrenaline in the adrenal medulla.肾上腺素和去甲肾上腺素在肾上腺髓质中的分布。
Nature. 1955 Jan 8;175(4445):88-9. doi: 10.1038/175088a0.