Hypertensive activity

A substituted thiazole ring attached to a reduced imidazole moiety is present in a compound that displays anti hypertensive activity. Reaction of thiourea 61 with methyl iodide to... 

The anticonvulsant effect, as well as the hypertensive activity of yohimbine have also been studied (343, 344). It has been shown that yohimbine produces significant increases in subjective anxiety, autonomic symptoms, and blood pressure (345). 

It is difficult to draw firm conclusions about the relevance of this central action of 3-blockers in animals to their clinical anti-hypertensive activity bearing in mind that brain concentrations of the different drugs varies widely... 

Xu, Q., Y. Liu, M. Gorospe, R. Udelsman, and NJ. Holbrook. 1996. Acute hypertension activates mitogen-activated protein kinases in arterial wall 2. J. Clin. Invest. 97 508-514. 

Takano, T. 2002. Anti-hypertensive activity of fermented dairy products containing biogenic peptides. Antonie van Leeuwenhoek 82, 333-340. 

The stem bark of P. yohimbe (= P. johimbe Corynanthe yohimbe), "yohimbe as it is known in Cameroon, Gabon and Congo is used traditionally as an aphrodisiac and stimulant to prevent sleep (41). The bark contains 1-6% of indole alkaloids, most of which are yohimbane-type alkaloids, the main one being yohimbine [7], which is structurally related to reserpine [8] (89). Yohimbine is a selective inhibitor of a-2- adrenergic receptors and, while at low dose it has hypertensive activity, at high dose it is hypotensive (vasodilation of peripheral vessels). It is the vasodilation of peripheral vessels, and especially vasodilation of the corpus cavemosum, which is the cause of the reputation of yohimbine as an aphrodisiac (90). Tests have shown, indeed, that increased... 

A similar study of the anti-hypertensive activity of the alkaloids of Kopsia teoi were also carried out which were also prompted by positive results from preliminary screening of alkaloidal extracts. The major aspidofractinine alkaloid kopsingine (191) was found to produce dose-related decreases in mean arterial blood pressure and heart rate in anaesthetized spontaneously hypertensive rats (SHR) which were similar to those elicited in normotensive controls. The same depressor response was shown by the 12-demethoxy derivative (kopsaporine, 192) and the semisynthetic 14,15-dihydto derivative of kopsingine 252, indicating that minor modifications to the basic structure of kopsingine do not significantly alter... 

This phenomenon is particularly observed when the buUdness of cationic heads is progressively increased. In N-alkylated derivatives of norepinephrineP progressive alkylation reduces the hypertensive activity according to the sequence NH2, NHMe, NHEt, NHNPro. Finally, the molecules become hypotensive for the values NHlsoPro, NHnBu and NHIsoBu (Table 14.4). 

Ru(NH3)4P(OEt)3(NO)](PF6)3 exhibits reduced toxicity and similar hypertensive activity compared with sodium nitroprusside, which is used to treat cardiovascular disorders in animal studies. This property is due to the strong trans effect of the P(OEt)3 ligand, which is responsible for the release of the NO group [57]. With trons-[RuCl(cyclam)(NO)](PF6)2, prolonged blood pressure reduction was observed (cyclam= 1,4,8,11-tetraazacyclotetradecane) [58]. 

The oligosaccharides prepared from alginate can exhibit a variety of biological activities, including anti-allergy properties, anti-hypertensive activity, an ability to enhance the growth of human endothelial cells and keratinocytes, and an ability to induce cytokine production [157]. 

Boublik,J.H., Scott, N.A., Brown, M.R. Rivier, J.E. (1989a) Synthesis and hypertensive activity of neuropeptide Y fragments and analogues with modified N- or C-termini of d-substitutions. J. Med. Chem. 32, 597-601. 

Similar conclusions could be derived from an investigation of antihypertensive clonidine analogs, with respect to their peripheral hypertensive side effects. For a series of clonidine-related imidazolines, log Papp values were determined in -octanol/buffer at pH 7.4, central antihypertensive activities C2s (molar doses that cause a 25% blood pressure decrease, intravenous application) in anesthesized rats, peripheral hypertensive activities C o (molar doses that cause a 60-mm Hg blood pressure increase, intravenous application) in pithed rats (i.e., rats without central nervous system control), binding affinities IC50ai to ai receptors (replacement of prazosin), and binding affinities IC50+ 10 a2 receptors (replacement of clonidine) [86,87],... 

Reaction of sulphamide 337 with a series of amines has led to the synthesis of 2-sulphamido-1.3,4.6.7,11b-2-hexahydro-2//-benzo[V]-quinolizines (349), R3 = NHS02NH2, and the anti-hypertensive activity of the compounds in rats has been reported355. 

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