Properties, antihypertensive

A series of hydroxystyrylisoxazoles have reported antiarrhythmia-antihypertensive properties (79GEP2818998). 

Forskolin (5-[acetyloxy]-3-ethenyldodecahydro-6,10,10b-trihydroxy-3,4a,7,7,10a-penta-methyl-[3R- 3a-4aP, SP, 6P, 6aa,10a, lOaP, 10ba -lFf-naphtho[2,l-b]pyran-l-one) [66575-29-9] M 410.5, m 229-232°, 228-233°. Recrystd from CfiH6-pet ether. It is antihypertensive, positive ionotropic, platelet aggregation inhibitory and adenylate cyclase activating properties [Chem AbstrS9 1978 244150, de Souza et al. Med Res Rev 3 201 1983]. 

Many alkaloids have pronounced biological properties, and a substantial number of the pharmaceutical agents used today are derived from naturally occurring amines. As a few examples, morphine, an analgesic agent, is obtained from the opium poppy Papaver somnifemm. Cocaine, both an anesthetic and a central nervous system stimulant, is obtained front the coca bush Erythroxylon coca, endemic to upland rain forest areas of Colombia, Ecuador, Peru, Bolivia, and western Brazil. Reserpine, a tranquilizer and antihypertensive, comes from powdered roots of the semitropical plant Rauwolfia serpentina. Ephedrine, a bronchodilator and decongestant, is obtained front the Chinese plant Ephedra sinica. 

Barriault developed a new pericyclic domino process for the synthesis of the bioactive diterpenoid vinigrol (4-262), which was isolated from Vtrgaria nigra [92]. The natural product possesses antihypertensive and anti-platelet-aggregating properties. 4-262 contains a unique tricyclo [4.4.4.04a8a]tetradecane framework, which could be obtained by a combination of an oxy-Cope, a Claisen and an ene reaction... 

Potassium-sparing diuretics are weak antihypertensives when used alone but provide an additive hypotensive effect when combined with thiazide or loop diuretics. Moreover, they counteract the potassium- and magnesiumlosing properties and perhaps glucose intolerance caused by other diuretics. 

Mesoionic oxatriazolium-5-amenates 83 exhibit the whole range of biological properties typical of NO-releasing compounds that stimulate soluble guanylate cyclase namely antihypertensive activity in animals following the relaxation of the vascular... 

The medicinal chemist expects to find that a review written specifically for him will he mainly concerned with a discussion of structure/activity relationships. In the case of the antihypertensive activity of the (3-blockers such a discussion is not possible since no direct comparative activity data is available either from the laboratory or the clinic (the few comparative clinical studies are in no way definitive - see later). It is however possible to approach the problem somewhat indirectly and consider the influence of chemical structure on those pharma -cological properties which appear most relevant to the specific clinical effect. I propose therefore to -... 

Triamterene is also a diuretic with distal tubule action and potassium retaining properties. It is not generally used alone as an antihypertensive agent. 

The thiazide diuretics possess antihypertensive properties, in part consequent upon electrolyte and plasma-volume changes but mainly resulting from a direct cardiovascular depressant effect. This is clearly illustrated by the non-diuretic thiazide, diazoxide, which is an effective hypotensive [326b, c]. It is not therefore, surprising that both these properties should be found (in varying proportions) in other, structurally related, compounds. One particular line of research, aimed at modification of the thiazide heterocycle (the o-chlorobenzenesulphonamide moiety was untouched as it was believed essential to activity-the subsequent advent of ethacrynic acid questions this belieO examined first the corresponding... 

There is no correlation between the monoamine oxidase inhibitory activity of guanidine derivatives and their ability to cause adrenergic neurone blockade or depletion of noradrenaline [259]. The contribution made by monoamine oxidase inhibition to the antihypertensive properties of guanidines remains to be... 

Ephedra (Ephedra sinica)/Ma Huang Uses Stimulant, aid in wt loss, bronchial dilation Dose Not OK d/t reported deaths (>100 mg/d can be life-threatening). US sales banned by FDA in 2004 bitter orange w/ similar properties has replaced this compound in most wt loss supplements Caution Advise cardiac events, strokes, death SE Nervousness, HA, insomnia, palpitations, V, hypoglycemia Interactions Digoxin, antihypertensives, antidepressants, diabetic medications EMS Tinctures extracts contain EtOH may X glucose linked to several deaths behavioral mood changes... 

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