Antihypertensive agents 3-adrenoceptor antagonists

More then a dozen representatives of the above ring systems were introduced into the human therapy. Actisomide (2) and trequinsin (3) are used as antiarrhytmic and antihypertensive agents, respectively. Sunepitron (4), a a 2-adrenoceptor antagonist, is under clinical trials for the treatment of anxiety and depression. Representatives of the third generation of antibacterial quinolone-3-carboxylic acids the blockbluster ofloxacin (5), its levorotatory enantiomer, levofloxacin (6), and rufloxacin (7) have gained wide acceptance for the treatment of bacterial infections of the respiratory and urinary tracts, skin, and soft tissues, as well as sexually transmitted diseases, and pazufloxacin (8) is under development. Praziquantel (9) is widely applied for the treatment of schistosomes- and cestode-caused infection in both veterinary and human therapies (Scheme 4). 

The renaissance of the Biginelli MCR can be attributed to the obtained pyrimidine derivatives, which show remarkable pharmacological activity. A broad range of effects, including antiviral, antitumor, antibacterial, anti-inflammatory as well as antihypertensive activities has been ascribed to these partly reduced pyrimidine derivatives [96], such as 9-117 and 9-118 (antihypertensive agents) [97] and 9-119 (ala-adrenoceptor-selective antagonist) [98] (Scheme 9.24). Recently, the scope of this pharmacophore has been further increased by the identification of the 4-(3-hydroxyphenyl)-pyrimidin-2-thione derivative 9-120 known as monastrol [98], a novel cell-permeable lead molecule for the development of new anticancer drugs. Monastrol appears specifically to affect cell division (mitosis) by a new mechanism,... 

Alabaster, V.A., Campbell, S.F., Danilewicz, J.C., Greengrass, C.W. and Plews, R.M. (1987) 2,4-Diamino-6,7-dimethoxyquinazolines. 2.2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. Journal of Medicinal Chemistry, 30, 999—1003. 

Diamino-6,7-dimethoxyquinazolines. 3.2-(4-Heterocyclylpiperazin-l-yl) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. Journal of Medicinal Chemistry, 30, 1794-1798. 

Selective a i-adrenoceptor antagonists are among the few antihypertensive agents that moderately improve the plasma lipid profile, glucose tolerance... 

Yohimbe bark Centrally active antihypertensive agents Yohimbine (a major alkaloid in yohimbe bark) may antagonize guanabenz and the methyldopa metabolite through its oj-adrenoceptor antagonistic properties. 

Antihypertensive Agents. Hypertension (high blood pressure) is a significant risk factor for cardiovascular diseases such as angina heart attacks, and strokes. /(-Adrenoceptor (adrenergic nervous system receptors of the /(-type) antagonists (/(-blockers), calcium channel blockers, angiotensinconverting enzyme (ACE) inhibitors, and potassium channel activators... 

Alpha-adrenoceptor antagonists are useful antihypertensives they block the vasoconstrictor effects of a-receptor stimulation. There is sometimes a problem with postural hypotension as reflexes which normally raise BP on standing are interrupted. These agents have a beneficial effect on blood lipids. 

Narayan P, Man In t Veld AJ. Clinical pharmacology of modern antihypertensive agents and their interaction with alpha-adrenoceptor antagonists. Br J Urol 1998 81(Suppl 1) 6-16. 

Salt and fluid retention is an adverse effect of indometacin, although it is less important than with the pyrazolone derivatives. Indometacin can antagonize antihypertensive agents, including beta-adrenoceptor antagonists (19,20). The effect on blood pressure in normotensive patients has not been adequately studied. 

Levatol ) is a (subtype-non-selective) P-adrenoceptor ANTAGONIST. It can be used as an antihypertensive. penbutolol sulfate penbutolol. penciclovir [ban, inn] (Vectavir ) is a synthetic nucleoside analogue antiviral, used topically as a treatment for herpes infections. It can also be used orally in the form of its prodrug famciclovir. It is active as an anti-hiv agent. Pendramine penicillamine. 

U 8344) is derived from mustine, and is an alkylating anti-CANCER AGENT used orally to treat lymphomas and leukaemias, urapidil [ban.inn.jan] is a novel piperazinyl pyrimidinedione derivative with mixed ( i-subtype) a-ADRENOCEPTOR ANTAGONIST, CNS and (5-HTia) 5-HYDROXYTRYPTAMINE RECEPTOR ANTAGONIST properties. It has been used as an antihypertensive. urea [usan] (carbamide) is a constituent of ail vertebrate tissues, concentrated in urine. It can be used topically as a... 

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