Hypotensive agents

As we have had occasion to note more than a few times previously, the guanidine function forms the basis of a family of hypotensive agents active by reason of their activity as blockers of the peripheral sympathetic system. Condensation of tetra-hydroisoquinoline with the S-methyl ether of thiourea affords the antihypertensive drug debrisoquin (135). ... 

An imidazole derivative which is also a hypotensive agent by virtue of adrenergic a-2-receptor blockade is imiloxan (75). Its synthe.sis begins by conversion of 2-cyanomethyl-1,4-benzodioxane (72) to its iminosMhylether with anhydrous HC in clhanol (73). Reaction of the latter with aminoacetaldehyde diethylacetal and subsequent acid treatment produces the imidazole ring (74). Alkylation of 74 with ethyl iodide mediated by sodium hydride completes the synthesis [251. 

Mollusca and Arthropoda. A variety of pharmacological actions are induced by the toxins found in molluscs (17). For example, surugatoxin is a potent mydriatic (5J), ganglion blocker (84), and a potent hypotensive agent in cats. 

Quinuclidinol 1619-34-7 Hypotensive agent Probably used in synthesis of pharmaceuticals BZ 2.65... 

Displacement of halogen by ammonia leads to the corresponding amine, probably by an addition-elimination mechanism. There is thus obtained amquinsin (10), a hypotensive agent. Formation of the Shiff base of amquinsin with veratraldehyde gives leniquinsin (11),5 possibly a prodrug. 

Derivatives 82 (R=cycloalkyl) proved to be central nervous system stimulants, whereas 3-alkyl analogs were claimed as vasodepressant or hypotensive agents with some residual central nervous system activity [139, 154]. 

Presently on the U.S. market there are three compounds commonly considered as peripheral dilating hypotensive agents. These are hydralazine (I), placed on the market in 1953 by CIBA, diazoxide (II) from Schering in 1973 and sodium nitroprusside (III) made available by Roche in 1974. 

An enzyme inhibitor of microbial origin with a simple structure, fusaric acid (XXXIV), is a hypotensive agent. This compound has been tested clinically as the free acid (29) and as the calcium salt (30) and is orally effective in man with a low incidence of side-effects. Dopamine-p-hydroxylase inhibitory action of this compound has been demonstrated in man (29). 

Hypotensive agents—Congresses. 2. Adrenergic beta receptor blockaders—Congresses. 

Welcome [67,68]. Bethanidine was initially patented as a hypotensive agent but was found to have antifibrillatory activity [69]. Attempts to limit the hypotensive effects of bethanidine led to meobentine. At a concentration of 44 fxM, bethanidine has minimal effects on APDioo in propranolol-treated and untreated canine Purkinje fibres (-1-2% and —5%, respectively) [70,71], At 350 //M in untreated fibres, bethanidine increased APDioo t>y about 6%. In contrast, meobentine, which has less sympatholytic activity, increased APDioo t>y 12% at 37 //M in untreated fibres during the same study. Both compounds showed modest decreases of V ax at the stated concentrations. The Class I activity and the sympatholytic activity (for bethanidine) may act to decrease the apparent Class III effects of the two compounds (see below). 

Halogen-substituted T,2, 3, 4 -tetrahydro-l-naphthyl-1,4,5,6-tetrahydropyri-midines, such as (XCVll), and their non-toxic water-soluble salts, are useful as hypotensive agents [681] 2-(p-Aminophenyl)-l,4,5,6-tetrahydropyrimidines (XCVlll), prepared from p-aminobenzoic acid ester and a,co-diaminoalkanes, are active as local anaesthetics over a wide pH range [682]. 

Hydroxylation, osmium tetroxide, 138 Hypoglycemics, oral, 20 Hypotensive agent, 5... 

The relation between the dosage, plasma concentration, and hypotensive action of hydrallazine has recently been examined (Zl). This drug, despite its many advantages as a hypotensive agent, fell from favor because of an unacceptably high incidence of severe side effects. Studies by Perry et al. (P8) have shown, however, that slow acetylators are more liable to develop the severe lupuslike syndrome associated with hydrallazine usage than fast acetylators. 

Some 3-substituted anhydro-5-hydroxy-l,2,3,4-oxatriazolium hydroxides (4), anhydro-5-thiolo-1,2,3,4-oxatriazolium hydroxides (5) and anhydro-5-amino-l,2,3,4-oxatriazolium hydroxides (6) possess pesticidal or herbicidal properties <79BRP2015878>. Anhydro-5-hydroxy-l,2,3,4-oxatria-zolium hydroxides (4) are moderately active but relatively long-acting hypotensive agents <82JMC1503>. 

Ac) and the salts (285) have been claimed as hypotensive agents. 

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