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Spontaneously hypertensive rat

Cromakalim (137) is a potassium channel activator commonly used as an antihypertensive agent (107). The rationale for the design of cromakalim is based on P-blockers such as propranolol (115) and atenolol (123). Conformational restriction of the propanolamine side chain as observed in the cromakalim chroman nucleus provides compounds with desired antihypertensive activity free of the side effects commonly associated with P-blockers. Enantiomerically pure cromakalim is produced by resolution of the diastereomeric (T)-a-meth5lben2ylcarbamate derivatives. X-ray crystallographic analysis of this diastereomer provides the absolute stereochemistry of cromakalim. Biological activity resides primarily in the (—)-(33, 4R)-enantiomer [94535-50-9] (137) (108). In spontaneously hypertensive rats, the (—)-(33, 4R)-enantiomer, at dosages of 0.3 mg/kg, lowers the systoHc pressure 47%, whereas the (+)-(3R,43)-enantiomer only decreases the systoHc pressure by 14% at a dose of 3.0 mg/kg. [Pg.253]

The antihypertensive activity of 8-aryl-6,9n-dimethyl-2,3,4,8,9,9n-hexahy-dropyrido[2,l-Z)][l,3]oxazine-7,9-dicarboxylates 79 was evaluated in conscious spontaneously hypertensive rats. They resulted in potent and long-lasting antihypertensive action (97MI14). [Pg.189]

Hamet, P., Kong, D., Pravenec, M., Kunes, J., Kren, V., Klir, P., Sun, Y.L., Tremblay, J. (1992). Restriction fragment length polymorphism of hsp70 gene, localized in the RTl complex, is associated with hypertension in spontaneously hypertensive rats. Hypertension 19,611-614. [Pg.454]

Hashimoto, T., Mosser, R.D., Tremblay, J., Hamet, P. (1991). Increased accumulation of hsp70 mRNA due to enhanced activation of heat shock transcription factor in spontaneously hypertensive rats. J. Hyperten. Suppl. 9, S170-171. [Pg.455]

UCHIDA S, OZAKI M, KASHI T, YAMASHITA K, NIWA M and TANIYAMA K (1995) Effects of (-)-epigallocatechin-3-O-gallate (green tea tannin) on the life span of stroke-prone spontaneously hypertensive rats , Clin Exp Pharmacol, 11 (Suppl 1), S302-303. [Pg.157]

The antioxidant property of ferulic acid and related compounds from rice bran was reported by Kikuzaki et al, (2002). Their results indicated that these compounds elicit their antioxidant function through radical scavenging activity and their affinity with lipid substrates. Another recent study reported by Butterfield et al, (2002) demonstrated that ferulic acid offers antioxidant protection against hydroxyl and peroxyl radical oxidation in synaptosomal and neuronal cell culture systems in vitro. The effect of ferulic acid on blood pressure (BP) was investigated in spontaneously hypertensive rats (SHR). After oral administration of ferulic acid the systolic blood pressure (SBP) decreased in a dose-dependent manner. There was a significant correlation between plasma ferulic acid and changes in the SBP of the tail artery, suggesting... [Pg.361]

ICHIRO T, AKIHIKO, F, DAiJi K, RYUJi o, IKUO s, ATSUSHi s (2002) Short and long term effects of ferulic acid on blood pressure in spontaneously hypertensive rats. American J of Hypertension, 15(4) part 1 351-57. [Pg.372]

In contrast to the deleterious effects of arginine described by Buisson, L-arginine was shown to decrease infarct size caused by middle cerebral artery occlusion in spontaneously hypertensive rats. L-Arginine is a precursor for NO synthesis by NOS. The authors attributed the protection to dilation of cerebral blood vessels by NO (Morikawa et 1992). These examples illustrate the difficulty that the NO villain/protector paradox presents to us. [Pg.267]

SHR Spontaneously hypertensive rat SIM Selected ion monitoring SIRS Soluble immune response suppressor... [Pg.286]

ADHD Passive avoidance in spontaneously hypertensive rats Improves cognitive performance [57]... [Pg.183]

Ragolia, L., et al. (2003). Prostaglandin D2 synthase inhibits the exaggerated growth phenotype of spontaneously hypertensive rat vascular smooth muscle cells. J. Biol. Chem. 278, 22175-81. [Pg.384]

Kirsch T, Wellner M, Luft FC, Haller H, Li ppoldt A. Altered gene expression in cerebral capillaries of stroke-prone spontaneously hypertensive rats. Brain Res 2001 910 106-115. [Pg.335]

Napoli et al. [286] found that the nifedipine treatment of stroke-prone spontaneously hypertensive rats (SPSHR) suppressed the plasma and LDL oxidation and the formation of oxidation-specific epitopes and increased the survival of rats independently of blood pressure modification. Their results suggest that the protective effects of calcium blockers of dihydro-pyridine-type on cerebral ischemia and stroke may, at least in part, depend on their antioxidant activity. In vivo antioxidant effect of nilvadipine on LDL oxidation has been studied in hypertensive patients with high risk of atherosclerosis [287], It was found that there was a significant decrease in the level of LDL cholesterol oxidation in patients after nilvadipine treatment. [Pg.884]

Wiessner, C., Bareyre, F. M., Allegrini, P. R. etal. Anti-Nogo-A antibody infusion 24 hours after experimental stroke improved behavioral outcome and corticospinal plasticity in normotensive and spontaneously hypertensive rats. J. Cereb. Blood Flow Metab. 23 154-165, 2003. [Pg.527]

Pascual, D.W. et al., Nitric oxide mediates immune dysfunction in the spontaneously hypertensive rat, Hypertension, 21, 185, 1992. [Pg.181]

Arii T, Ohyanagi M, Shibuya J, Iwasaki T 1999 Increased function of the voltage-dependent calcium channels, without increase of Ca2+ release from the sarcoplasmic reticulum in the arterioles of spontaneous hypertensive rats. Am J Hypertens 12 1236-1242 Attree O, Olivos IM, Okabe I et al 1992 The Lowe s oculocerebrorenal syndrome gene encodes a protein highly homologous to inositol polyphosphate-5-phosphatase. Nature 358 239-242 Brading AF, Turner WH 1994 The unstable bladder towards a common mechanism. Br J Urol 73 3-8... [Pg.252]

Nomura Y, Asano M, Ito K, Uyama Y, Imaizumi Y, Watanabe M 1997 Potent vasoconstrictor actions of cyclopiazonic acid and thapsigargin on femoral arteries from spontaneously hypertensive rats. Br J Pharmacol 120 65—73... [Pg.253]

All products showed antithrombotic activity the most potent was found to be the dimethyl derivative, which also significantly decreased blood pressure when administered orally to spontaneously hypertensive rats. Possible involvement of NO in this action was suggested but not demonstrated. [Pg.169]

Some optically active compounds have been studied [54], The benzazepinone diacid (CGS 12831, 27) was found to have the best in vitro inhibitor potency in a series of lactam compounds, but it showed only marginal biological activity following oral administration, presumably because of poor absorption. The corresponding monoethyl ester (CGS 14824A, 28) was much more potent in vivo [54, 56]. This compound (28) was found to produce dose-dependent antihypertensive effects in conscious normotensive and spontaneous hypertensive rats, generally similar to those produced by enalapril. Evaluation of (28) in healthy volunteers [57, 58] shows that it is an effective,... [Pg.132]

Figure 28. Influence of an additional methyl group in derivatives of methyldopa on the blood pressure lowering activity in spontaneously hypertensive rats... Figure 28. Influence of an additional methyl group in derivatives of methyldopa on the blood pressure lowering activity in spontaneously hypertensive rats...
A mesoionic compound PR-G-138-C1 (XXXIX) from Pharma Research in Canada is reported to lower blood pressure in man at low doses by a vasodilator type mechanism (43). This structure is related to SIN-10 (XL) which was reported earlier by Japanese scientists as active in dogs (44). Compounds related to structure XXXIX were compared in spontaneous hypertensive rats and those with the oxadiazole ring hydrogen replaced by chlorine or bromine were as active as the parent compound, although replacement by methyl caused a loss of activity (45). [Pg.63]

Maruyama, H., Sumitou, Y., Sakamoto, T., Araki, Y. and Hara, H. (2009) Biol. Pharm. Bull., Antihypertensive effects of flavonoids isolated from Brazilian green propolis in spontaneously hypertensive rats, 32(7), 1244-1250. [Pg.109]

H. Sanada, L. D. Asico, S. Shigetomi, K. Tanaka, S. Niimura, H. Watanabe, D. S. Goldstein, R. A. Felder, The Effect of Docarpamine, a Dopamine Prodrug, on Blood Pressure and Catecholamine Levels in Spontaneously Hypertensive Rats , Clin. Exp. Hyper-tens. 2000, 22, 419 - 429. [Pg.370]

Sunderland T, Tariot PN, Newhouse PA. (1988). Differential responsivity of mood, behavior, and cognition to cholinergic agents in elderly neuropsychiatric populations. Brain Res. 472 4y. 371-89. Tachikawa E, Kudo K, Flarada K, Kashimoto T, Miyate Y, Kakizaki A, Takahashi E. (1999). Effects of ginseng saponins on responses induced by various receptor stimuli. EurJ Pharmacol 369(1) 23-32. Tagami M, Ikeda K, Yamagata K, Nara Y, Fujino FI, Kubota A, Numano F, Yamori Y. (1999). Vitamin E prevents apoptosis in hippocampal neurons caused by cerebral ischemia and reperfusion in stroke-prone spontaneously hypertensive rats. Lab Invest. 79(5) 609-15. [Pg.490]

In the United States also, 5,6-diarylpyridazinone derivatives have been studied extensively as potential antihypertensive agents [374-377]. From experiments with spontaneously hypertensive rats and the deoxycorticosteroid model of hypertension, it turned out that substitution of the phenyl rings by halogen, introduction of an electron-attracting group (like acetyl or... [Pg.160]

Tanaka M, Matsni T, Ushida Y, Matsumoto K. (2006) Vasodilating effect of di-peptides in thoracic aortas from spontaneously hypertensive rats. Biosci Biotechnol Biochem 70 2292-2295. [Pg.216]

Eujita H, Yamagami T, Ohshima K. (2001) Effects of an ACE-inhibitory agent, katsuobushi oligopeptide, in the spontaneously hypertensive rat and in borderline and mildly hypertensive subjects. Nutr Res 21 1149-1158. [Pg.217]

Lee SH, Qian ZJ, Kim SK. (2010) A novel angiotensin 1 converting enzyme inhibitory peptide from tuna frame protein hydrolysate and its antihypertensive effect in spontaneously hypertensive rats. Food Chem 118 96-102. [Pg.218]

Matsui T, Imamura M, Oka H, Osajima K, Kimoto K, Kawasaki T, Matsumoto K. (2004) Tissue distribution of anti-hypertensive dipeptide, Val-Tyr, after its single oral adnunistration to spontaneously hypertensive rats. J Pept Sci 10 535-545. [Pg.219]

Masnda O, Nakamura Y, Takano T. (1996) Anti-hypertensive peptides are present in aorta after oral administration of sour milk containing these peptides to spontaneously hypertensive rats. JNutr 126 3063-3068. [Pg.219]


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