• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.220-225
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• 1993

Effect of BR-900317 on the angiotensin I-induced pressor response in pithed rats and the effects of its single oral administration on plasma angiotensin converting enzyme (ACE) activities in normotensive rats and on the cardiovascular system in hypertensive model rats (SHR, RHR), were compared with those of captopril. BR-900317 attenuated the angiotensin I-induced pressor effects in pithed rats. In a single oral dose administration study, BR-900317 inhibited the plasma ACE activities in a dose-dependent fashion. Duration of the action of BR-900317 was similar to that of captopril. BR-900317 produced antihypertensive effect in spontaneously hypertensive rats and dose-dependent antihypertensive effect in 2-kidney Goldblatt hypertensive rats without affecting heart rate. These results suggest that the main mechanism of the antihypertensive effect of BR-900317 is the suppression of angiotensin II production due to the inhibition of the ACE.

• Proceedings of the Korean Society of Fisheries Technology Conference
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• 2001.10a
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• pp.171-172
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• 2001

체내에 널리 분포되어 있는 angiotensin 전환효소(angiotensin converting enzyme, ACE ; peptidyldipeptide hydrolase, EC 3.4.15.1)는 angiotensinogen이 renin의 특이적 분해를 받아서 생성된 불활성형인 angiotensin I의 말단 dipeptide(His-Leu)를 절단하여 octapeptide인 활성형의 angiotensin II로 전환시키며, 이렇게 생성된 angiotensin II는 직접적으로 혈압상승 작용을 하거나 adrenal로부터 sediumretaining steroid hormone인 aldosterone의 유리를 촉진시켜 체내 나트륨을 저류시킨다. (중략)

• Korean Journal of Food Science and Technology
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• v.25 no.3
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• pp.238-242
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• 1993

For the Purpose of utilizing tannins in the functional foods and crude drugs, the enzyme inhibition of tannins isolated from Korean green tea were determined. Acetone extract from Korean green tea showed inhibition effect against the angiotensin converting enzyme. The galloyl tannins showed higher inhibition activity against angioteosin converting enzyme than the nongalloyl tannins. In terms of stereo isomers, (-)-epicatechins had higher inhibition activity than the (+ )-catechins. The synergistic activity was also observed. Tannins isolated from Korean green tea appeared to be incompetitive inhibitor against the angiotensin converting enzyme.

• The Korean Journal of Pharmacology
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• v.30 no.1
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• pp.75-86
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• 1994

To assess the role of adrenal medulla and renin-angiotensin system in the regulation of sympathetic neurotransmission, the pressor response to PNS was evaluated in pithed SHR and normotensive WKY or SDR with or without adrenal demedullation and/or enalapril pretreatment. Three weeks after adrenal demedullation, MAP and the heart rate of demedullated rats were similar to their corresponding sham-operated groups. The pressor response to PNS was frequency-dependent, and blocked by prazosin. In contrast to the normotensive rats, in SHR, the pressor response to PNS was attenuated in demedullated rats as compared with sham-operated rats. However, the attenuation of PNS-induced pressor responses in demedullated SHR was not observed in enalapril-treated SHR. The adrenal demedullation in SHR did not affect the plasma and aortic catecholamine contents in spite of the decreased catecholamine contents of adrenal gland, nor ACE activity in aortic strips. But, in WKY rats, the aortic catecholamines, especially epinephrine, contents as well as ACE activity were increased by adrenal demedullation. These results suggest that the facilitatory role of adrenal medulla in sympathetic neurotransmission depends upon the activation of renin-angiotensin system, and that the compensatory regulation of renin-angiotensin system takes place in normotensive rats but not in SHR.

• Journal of Pharmaceutical Investigation
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• v.19 no.4
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• pp.185-190
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• 1989

The release of angiotensin and ${\alpha}-amylase$ from monolithic devices of different molecular weight of polyethylene glycol (PEC) grafted polyurethane copolymer was investigated. Water-soluble PEG grafted polymer provided a controlled release of angiotensin and ${\alpha}-amylase$. The release rate of angiotensin and ${\alpha}-amylase$ could be controlled by varying the molecular weight of PEC grafted. The release mechanism may be associated with the creation of pore or domain through the devices following the gel swelling and self-aggregation by PEC grafted polymer. Hydrophobic polyurethane grafted with PEG can provide a biomaterial for prolonged release of angiotensin and ${\alpha}-amylase$ from angiotensin and ${\alpha}-amylase$ blended system.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.298-298
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• 1994

Norepinephrine이나 angotensin II가 그 작용을 나타내는데 $Ca^{+2}$의 세포내 유입 또는 유출과 밀접한 관련이 있다는 관점에서 $Ca^{+2}$ -channel차단제중 benzothiazenpine계인 diltiazem의 norepinephrine과 angiotensin II의 혈압상승작용에 대한 영향을 가토에서 관찰하였다. Norepinephrine과 angiotensin II의 혈압상승작용에 대한 diltiazem의 영향을 관찰하는 경우는 diltiazem을 투여한 일정시간후에 norepinephrine이나 angiotensin II을 투여하여 나타나는 혈압변화를 diltiazem투여전의 norepinephrine이나 angiotensin II의 혈압상승치와 비교 검토하였다. Diltiazem은 norepinephrine과 angiotensin II의 혈압상승작용을 억재하였으나 그 억제 시간은 지속적이지 않았다. 이와는 달리 diltiazem투여 30-40분에는 norepinephrine의 혈압상승작용의 강화현상이 나타났다. Diltiazem은 교감신경말단차단제인 bethanidine이나 신경절 차단제인 chlorisondamine 처리 가토에서도 norepinephrine이나 angiotensin II의 혈압상승작용을 억제하였다.

• Journal of Pharmaceutical Investigation
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• v.15 no.1
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• pp.22-31
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• 1985

The influence of some sympathetic blocking agents on pressor actions of norepinephrine and angiotensin was investigated in rabbits. 1. Phentolamine, sympathetic ${\alpha}-blocking$ agent, blocked the pressor action of norepinephrine, but did not affect the pressor action of angiotensin 2. Chlorisondamine, autonomic ganglionic blocking agent, potentiated the both actions of norepinephrine and angiotensin. 3. Guanethidine, bethanidine and debrisoquine, sympathetic neuronal blocking agents, potentiated the action of norepinephrine, while diminished that of angiotensin. 4. Reserpine, norepinephrine depleting agent, increased the pressor response of norepinephrine, but did not influence the pressor action of angiotensin.

• YAKHAK HOEJI
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• v.58 no.1
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• pp.16-20
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• 2014

KR-31064 was developed for the strong angiotensin II receptor antagonist among the one of pyridyl imidazol series compounds. To investigate the receptor-ligand binding characteristics of this nonpeptide antagonist, binding experiments were deployed in various conditions and ex vivo contractile responses were tested toward the standard compound, losartan. Receptor binding experiments with radiolabeled angiotensin II, the $IC_{50}$ value for KR-31064 resulted 0.67 nM without any activities toward type 2 angiotensin II receptor. The comparative potency against losartan was more than 18 fold and the specific activity in type 1 angiotensin II receptor was more than 10,000 fold comparing to the type 2 receptor. Scatchard analysis of saturation binding data showed KR-31064 acted on the receptor in a competitive mode. KR-31064 inhibited the contractile response derived by angiotensin II ($pK_B$: 9.86) similar to that of losartan with decreased maximum signals. As a potent and specific type 1 angiotensin II receptor antagonist, KR-31064 may have possibilities for the development of diagnostic ligands that can be used as tools for various biochemical research experiments and non-invasive diagnostics.

• Journal of Chest Surgery
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• v.32 no.4
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• pp.333-340
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• 1999

Background: Plasminogen activator inhibitor-1(PAI-1) is known as the primary physiological inhibitor of tissue-type plasminogen activator(t-PA) in the plasma, and is present within the atherosclerotic vessels. Increased plasma levels of PAI-1 are one of the major disturbances of the hemostatic system in patients with diabetes and/or hypertension, and may have multiple interrelations with the important risk factors in the development of atherosclerosis. This study was performed to determine whether altered gene expression of PAI-1 occurs within the arterial wall, and thereby potentially contributing to the increase of cardiovascular risks associated with diabetes and/or hypertension. Material and Method: The aortic vascular smooth muscle cells of the rat were exposed to 22 mM glucose, angiotensin II, and insulin increased PAI-1 mRNA expression with the use of Northern blotting were examined. Also examined were the effects of 22 mM glucose, angiotensin II and insulin on the growth of the rat's aortic smooth muscle cells by using MTT assay. Result: Twenty-two mM glucose treatment increased the PAI-1 mRNA expression in a time- and dose-dependent manner. Aniotensin II treatment synergistically increased the glucose-induced PAI-1 mRNA expression. In contrast, addition of insulin attenuated the increase of 22 mM glucose and angiotensin II induced PAI-1 mRNA expression. Furthermore, treatment of 22 mM glucose, angiotensin II and insulin resulted in a significant increase in cell numbers. This study demonstrated that 22 mM glucose and angiotensin II have a synergistic effect in stimulating the PAI-1 mRNA expression and in the cell growth of the rat's aortic smooth muscle cells. Conclusion: Elevation of glucose and angiotensin II may be important risk factors in impairing fibrinolysis and developing atherosclerosis in diabetic patients.

• Proceedings of the Korean Society of Fisheries Technology Conference
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• 2002.10a
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• pp.193-194
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• 2002

Angiotensin I converting enzyme (ACE) inhibitor was purified from Crassostrea gigas. The ACE belongs to the class of metalloprotease. This enzyme plays an important physiological role in regulating blood pressure of the rennin-angiotensin system by converting from angiotensin I to octapeptide angiotensin II, a potent vasoconstrictor and by inactivating bradykinin, which has depressor action. (omitted)