Selective receptor antagonist

Funk OF, Kettmann V, Drimal J, Langer T. Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists. J Med Ghent 2004 47 2750-60. 

Deslerotadine (Clarinex) [Antihislamine/Selective Receptor Antagonist] Uses Seasonal p ennial aU gic rhinitis chronic idiopathic urticaria Action Active metabohte of Claritin, Hpantihistamine, blocks inflammatory mediators Dose Adul Peds >12 y. 5 mg PO daily 5 mg PO qod... 

Fewer NK-3 selective receptor antagonists have been described, but a quinoline scaffold previously reported to be a selective NK-3 receptor antagonist, has been converted to a dual NK-2/NK-3 inhibitor (128) = 0.8 nM... 

TNF-a and increasing IL-8 (Webster et al., 2002). Consistent with this, selective receptor antagonists such as butox-amine can antagonize the corticotrophin-releasing factor-induced reduction in natural killer (NK) cell activity (Irwdn et al., 1990). Sympathetic nerve stimulation also enhances T 2 cytokine production while inhibiting cytokine production. Thus, pj receptor agonists can suppress interferon-y (IFN-y) production by cells, an effect, which can be blocked by propranolol. Interestingly, prion presence in the brain has been linked to an interaction between splenic monocytic cells and the sympathetic nervous system (Steinman, 2004). 

Confirmation that drug effects were mediated via CBi receptor activation was obtained through co-administration of the selective receptor antagonist rimonabant, which reversed deficits induced by A THC (Lichtman and Martin 1997 Mishima et al. 2001). Rimonabant alone had no effect when delays between entries 1-4 and 5-8 were short (Lichtman 2000 Lichtman and Martin 1997 Mishima et al. 2001), but there was a memory enhancement for delays of several hours (Lichtman 2000). This result suggests that blockade of CBi receptors may aid the development of short-term memory, and receptor antagonists may become important as cognitive enhancers not only for future animal research but also with respect to treatment of cognitive impairment in humans. 

More recently, the EPHESUS trial evaluated the effect of an aldosterone-selective receptor antagonist eplerenone in patients with... 

Urapidil is a selective receptor antagonist whose role in the treatment of hypertension remains to be determined. Urapidil is not available in the U.S. 

Ogletree, M., Allen, G., O Keefe, E., Liv, K. and Hedberg, A. (1986). Activities of various prostanoids at thromboxane receptors revealed by selective receptor antagonists Studies in human platelets and several rat and guinea-pig smooth muscles. In 6th International Conference on Prostaglandins, p. 350. (Fondazione Giovanni Lorenzini)... 

Darusentan is a propanoic acid-based endothelin type A-selective receptor antagonist that reduces blood pressure in patients with treatment-resistant hypertension. 

On the contrary, JNJ-37822681 (230) is a D2 highly selective receptor antagonist and hence acts in a mode analogous to that of most marketed antipsychotics [212], JNJ-37822681 is characterized by a rapid dissociation rate from the dopamine D2 receptor, which was hypothesized to confer antipsychotic efficacy and improved tolerability [213]. Clinical studies in patients with an acute exacerbation of schizophrenia showed that JNJ-37822681 had similar biological activity but lesser tendency to induce weight gain compared to a known antipsychotic drug. Olanzapine (242) [214] (Fig. 8). 

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