Competitive blocker antagonists

Competitive blocker of a-adrenergic receptors in heart and blood vessels Inhibits the enzyme HMG-CoA reductase and reduces the biosynthesis of cholesterol Acts as an angiotensin II receptor antagonist Inhibits the synthesis of prostaglandins via the selective inhibition of the enzyme cyclooxygenase-2... 

Pharmacology Histamine H2 antagonists are reversible competitive blockers of histamine at the H2receptors. They also inhibit fasting and nocturnal secretions, and secretions stimulated by food, insulin, caffeine, pentagastrin, and betazole. 

Ct9nACh-R (mixed n-m properties R) ACh-competitive blocker (mACh-R antagonist) [anticholinergic, anti-spasmodic, antidote to organophosphorous insecticide poisoning, mydriatic, toxic, vasodilatorv]... 

These results support the view that the blockade of NMDA receptor could be of therapeutic benefit, and, in this respect, glycine antagonists appear to be extremely effective. Furthermore, GV 150526 lacks the adverse behavioral effects in rats observed for both competitive NMDA antagonists and NMDA channel blockers neither... 

All of the muscarinic blockers, including scopolamine, act as reversible, competitive pharmacologic antagonists. The answer is (D). 

Competitive blocker A surmountable antagonist one that can be overcome by increasing the dose of agonist... 

A. Classiflcation, Subgroups, and Mecbanisms All of the clinically used beta-blockers are competitive phanuacologic antagonists. Propranolol is the prototype. Drugs in this group are usually classified into subgroups on the basis of P, versus P selectivity, partial agonist activity, local anesthetic action, and lipid solubility (Table 10-2). 

B. Mechanism and Effects H, blockers are competitive pharmacologic antagonists at the H, receptor these drugs have no effect on histamine release from storage sites. They are more effective if given before histamine release occurs. 

B, Mechanisms and Effects Ketanserin and cyproheptadine are competitive pharmacologic antagonists. Phenoxybenzamine is an irreversible blocker. 

Acid Pnmp Antagonists or Potassinm Competitive Acid Pnmp Blockers... 

Some antagonists combine the ability to block open ion channels with a competitive action at or near the agonist binding site. A well-characterized example is the nicotinic blocker tubocurarine (see Chapter 6). Agonists may also be open channel blockers, thus limiting the maximal response that they can elicit. Such agents (e g., decamethonium) may therefore behave as partial agonists when tested on an intact tissue ... 

When studying competitive antagonism, it is sometimes necessary to include an uptake inhibitor or a ganglion blocker in all the bathing solutions used. If this compound has in addition some competitive blocking action at the receptor being studied, what effect will this have on estimation of the dissociation equilibrium constant for a competitive antagonist ... 

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