新抗高血压药—血管紧张素ⅱ受体阻断剂的发展（New antihypertensive drugs, angiotensin II receptor blockers development）.docVIP

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新抗高血压药—血管紧张素ⅱ受体阻断剂的发展（New antihypertensive drugs, angiotensin II receptor blockers development）.doc

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新抗高血压药—血管紧张素ⅱ受体阻断剂的发展（New antihypertensive drugs, angiotensin II receptor blockers development）

新抗高血压药—血管紧张素ⅱ受体阻断剂的发展（New antihypertensive drugs, angiotensin II receptor blockers development） Development of a new antihypertensive drug angiotensin II receptor blocker Update Date: 2009-05-02 click: Pan Qichao Chen Yiqun Angiotensin II (Ang II) receptor blocker, fewer side effects, the advantages are not caused by depression, lack of concentration, do not interfere with sleep, do not make sexual dysfunction; II does not exacerbate heart failure, not bradycardia, peripheral vasoconstriction or nasal congestion, flushing and so on; 3 does not cause hypokalemia that does not cause hyperuricemia, hyperlipidemia, etc.; the non fluid retention, reflex heart rate and hypertension rebound; unlike the angiotensin converting enzyme inhibitor (ACE I) that cause cough. Therefore, it is a good antihypertensive drug. This kind of medicine is now: losartan (Losartan, Losartan, LOS), Stan (Valsartan VAL, spent Chastain), eprosartan (Eprosartan, Epro) and irbesartan (Irbesartan, Irbe) listed. The development of such drugs is outlined below. 1 mechanism of action This drug is blocking the receptor, which induced by Ang II: direct vascular contraction; the secretion of adrenaline and excitement of vasoconstriction; through aldosterone secretion caused by sodium and water retention, increase blood volume, thereby raising blood pressure induced by blocking, anti hypertension to achieve. 2 drug structure Chemically, a variety of drugs have similar structures, but all contain nitrogen heterocycles, and some contain butyl imidazole groups. 3 pharmacological effects 3.1 receptor binding assay The binding of 125I-Ang to 3.1.1 or II in rat liver or adrenal membrane is demonstrated by Epro, VAL, and IrbeLOS. 3.1.2 blocks 125I-Ang II binding on rat or rabbit aortic smooth muscle to prevent contraction, and Epro, LOS, and Irbe have been shown. AT1 cells in the adrenal gland membrane of 3.1.3 rats were inactivated by two sulfur dioxide, but Irbe and LOS did not bind, but Saralasin still combin