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酮色林对自发性高血压大鼠慢性5-羟色胺(5-HT2)受体阻滞的降压作用

Antihypertensive effects of chronic 5-hydroxytryptamine (5-HT2) receptor blockade with ketanserin in the spontaneously hypertensive rat.

作者信息

Pettersson A, Persson B, Henning M, Hedner T

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1984 Aug;327(1):43-7. doi: 10.1007/BF00504990.

DOI:10.1007/BF00504990
PMID:6493349
Abstract

The effects of chronic oral treatment with the 5-hydroxytryptamine (serotonin) receptor blocking agent ketanserin (17 mg/100 g dry food) on blood pressure, heart weight, peripheral vascular reactivity, baroreceptor sensitivity, central cardiovascular reactivity and central catecholamine turnover were investigated in the spontaneously hypertensive rat. Blood pressure measurements were performed in conscious rats 24 h after insertion of catheters. After 6 weeks treatment basal blood pressure was reduced (16%) compared to control rats (given identical food, except for ketanserin). Both heart weight and body weight were reduced (both to 93% of control values) leaving heart weight/body weight ratio unchanged. Pressor responses to phenylephrine and depressor responses to isoprenaline (after pretreatment with reserpine and atropin) were not different while the blood pressure increase to 5-hydroxytryptamine was inhibited, indicating that after 6 weeks treatment the blood pressure reduction is not directly related to alpha-adrenoceptor blockade. Cardiovascular response to stress (jet air), baroreceptor sensitivity (bradycardia to phenylephrine) and central catecholamine synthesis rates (accumulation of 5-hydroxytryptophan and dihydroxyphenylalanine after synthesis inhibition) were unchanged supporting earlier evidence that central mechanisms probably do not contribute to the hypotensive effects of ketanserin.

摘要

在自发性高血压大鼠中,研究了5-羟色胺(血清素)受体阻断剂酮色林(17毫克/100克干粮)长期口服治疗对血压、心脏重量、外周血管反应性、压力感受器敏感性、中枢心血管反应性和中枢儿茶酚胺周转率的影响。在有意识的大鼠插入导管24小时后测量血压。治疗6周后,与对照大鼠(给予除酮色林外相同的食物)相比,基础血压降低(16%)。心脏重量和体重均降低(均降至对照值的93%),而心脏重量/体重比不变。对去氧肾上腺素的升压反应和对异丙肾上腺素的降压反应(在用利血平和阿托品预处理后)没有差异,而对5-羟色胺的血压升高受到抑制,这表明治疗6周后血压降低与α-肾上腺素能受体阻断没有直接关系。对压力(喷气)的心血管反应、压力感受器敏感性(对去氧肾上腺素的心动过缓)和中枢儿茶酚胺合成率(合成抑制后5-羟色氨酸和二羟基苯丙氨酸的积累)没有变化,这支持了早期的证据,即中枢机制可能对酮色林的降压作用没有贡献。

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1
Antihypertensive effects of chronic 5-hydroxytryptamine (5-HT2) receptor blockade with ketanserin in the spontaneously hypertensive rat.酮色林对自发性高血压大鼠慢性5-羟色胺(5-HT2)受体阻滞的降压作用
Naunyn Schmiedebergs Arch Pharmacol. 1984 Aug;327(1):43-7. doi: 10.1007/BF00504990.
2
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J Cardiovasc Pharmacol. 1985;7 Suppl 7:S110-1. doi: 10.1097/00005344-198500077-00031.
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Antihypertensive effects of ketanserin and ritanserin in the spontaneously hypertensive rat.酮色林和利坦色林对自发性高血压大鼠的降压作用。
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Antihypertensive effects of chronic 5-hydroxytryptamine (5-HT2) receptor blockade with irindalone in the spontaneously hypertensive rat.在自发性高血压大鼠中,使用茚达立酮长期阻断5-羟色胺(5-HT2)受体的降压作用。
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Chronic 5-HT2 receptor blockade with ritanserin does not reduce blood pressure in the spontaneously hypertensive rat.用利坦色林进行慢性5-羟色胺2受体阻断不会降低自发性高血压大鼠的血压。
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Effects of antagonists of 5-hydroxytryptamine on blood pressure in the anesthetised spontaneously hypertensive rat.5-羟色胺拮抗剂对麻醉的自发性高血压大鼠血压的影响。
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Cardiovascular profile and hypotensive mechanism of ketanserin in the rabbit.
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An investigation of the effects of intravenous injection of the 5-hydroxytryptamine 2 receptor antagonists ketanserin and LY 53857 on blood pressure in anesthetized spontaneously hypertensive rats.静脉注射5-羟色胺2受体拮抗剂酮色林和LY 53857对麻醉的自发性高血压大鼠血压影响的研究。
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本文引用的文献

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Effect of alpha-methyl-3,4-dihydroxyphenylalanine (methyldopa), reserpine and related agents on some vascular responses in the dog.α-甲基-3,4-二羟基苯丙氨酸(甲基多巴)、利血平及相关药物对犬某些血管反应的影响。
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The antihypertensive effects of a pure and selective serotonin-receptor blocking agent (R 41 468) in elderly patients.一种纯的选择性血清素受体阻断剂(R 41 468)对老年患者的降压作用。
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Renal function and sympathetic activity during mental stress in normotensive and spontaneously hypertensive rats.
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Antihypertensive effect of long term ketanserin in elderly essential hypertensive patients. Assessment of left ventricular function at rest and during exercise.长期使用酮色林对老年原发性高血压患者的降压作用。静息及运动时左心室功能评估。
Drugs. 1988;36 Suppl 1:110-3. doi: 10.2165/00003495-198800361-00020.
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Antihypertensive mechanism of action of ketanserin and some ketanserin analogues in the spontaneously hypertensive rat.酮色林及一些酮色林类似物在自发性高血压大鼠中的降压作用机制
Naunyn Schmiedebergs Arch Pharmacol. 1985 Jun;329(4):394-7. doi: 10.1007/BF00496374.
6
Chronic 5-HT2 receptor blockade with ritanserin does not reduce blood pressure in the spontaneously hypertensive rat.用利坦色林进行慢性5-羟色胺2受体阻断不会降低自发性高血压大鼠的血压。
J Neural Transm. 1985;64(2):145-9. doi: 10.1007/BF01245975.
7
Pharmacokinetics of ketanserin in patients with cirrhosis.酮色林在肝硬化患者中的药代动力学。
Clin Pharmacokinet. 1990 Aug;19(2):160-6. doi: 10.2165/00003088-199019020-00005.
8
Antihypertensive effects of chronic 5-hydroxytryptamine (5-HT2) receptor blockade with irindalone in the spontaneously hypertensive rat.在自发性高血压大鼠中,使用茚达立酮长期阻断5-羟色胺(5-HT2)受体的降压作用。
J Neural Transm Gen Sect. 1991;83(3):227-33. doi: 10.1007/BF01253392.
正常血压和自发性高血压大鼠在精神应激期间的肾功能和交感神经活动
Acta Physiol Scand. 1982 May;115(1):115-24. doi: 10.1111/j.1748-1716.1982.tb07053.x.
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5-hydroxytryptamine and vascular disease.5-羟色胺与血管疾病
Fed Proc. 1983 Feb;42(2):233-7.
5
5-hydroxytryptamine and platelet aggregation.5-羟色胺与血小板聚集
Fed Proc. 1983 Feb;42(2):228-32.
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Ketanserin in essential hypertension: effects during rest and exercise.酮色林治疗原发性高血压:静息和运动时的效果
Eur J Clin Pharmacol. 1983;25(3):307-12. doi: 10.1007/BF01037939.
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Ketanserin, a novel 5-hydroxytryptamine antagonist: monotherapy in essential hypertension.酮色林,一种新型5-羟色胺拮抗剂:用于原发性高血压的单一疗法。
Br J Clin Pharmacol. 1983 Aug;16(2):121-5. doi: 10.1111/j.1365-2125.1983.tb04974.x.
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Experience with ketanserin, a serotonin (S2) antagonist, in longterm treatment of essential hypertension.酮色林(一种5-羟色胺[S2]拮抗剂)用于原发性高血压长期治疗的经验。
Clin Exp Hypertens A. 1984;6(3):743-51. doi: 10.3109/10641968409044035.
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Characterization of the antihypertensive properties of ketanserin (R 41 468) in rats.酮色林(R 41 468)对大鼠降压特性的表征
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Receptor binding profile of R 41 468, a novel antagonist at 5-HT2 receptors.新型5-羟色胺2受体拮抗剂R 41 468的受体结合情况
Life Sci. 1981 Mar 2;28(9):1015-22. doi: 10.1016/0024-3205(81)90747-5.