H -antagonism

Inhibition of Bezold-Jarisch reflex in rats. h Antagonism of cisplatin-induced emesis in ferrets and dogs. c L.M. Pinkus, personal communication. 

Huang Y, Lu M, Wu H. Antagonizing XIAP-mediated caspase-3 inhibition. Achilles heel of cancers Cancer Cell 2004 5 1-2. 

Doll DC, Rosenberg H. Antagonism of neuromuscular blockage by theophylline. Anesth Analg 1979 58(2) 139-40. 

A patent (95JAP07196655) deseribed the preparation of a 2//-indazole derivative of speeifie formula 109 useful as a therapeutie agent for a eireulatory disease sueh as hypertension, having angiotensin II antagonism and antihypertensive aetion. In formula 109 r = lower alkyl or alkenyl R, R = H, halogen, lower... 

Zhang, M., van de Stolpe, A., Zuiderveld, O., and Timmermans, H. (1997). Combined antagonism of leuko-trienes and histamine produces predominant inhibition of allergen-induced early and late phase airway obstraction in asthmatics. Eur. J. Med. Chem. 32 95—102. 

Williams SA, Chen LF, Kwon H, Fenard D, Bisgrove D, Verdin E, Greene WC. Prostratin antagonizes HIV latency by activating NF-kB. J Biol Chem 2004 279 42008-17. 

Chalasani SH, Sabol A, Xu H, Gyda MA, Rasband K, Granato M, Chien CB, Raper JA (2007) Stromal cell-derived factor-1 antagonizes slit/robo signaling in vivo. J Neurosci 27 973-980... 

PATISAUL H B, DiNDO M, WHITTEN p L, YOUNG L J (2001) Soy isoflavone Supplements antagonize reproductive behavior and oestrogen receptor alpha- and beta-dependent gene expression in the brain. Endocrinol. 142 2946-52. 

Miczek, K.A., and Yoshimura, H. Disruption of primate social behavior by (/-amphetamine and cocaine Differential antagonism by antipsychotics. Psychopharmacology 76 163-171, 1982. 

The above conclusion is supported by the results shown in figure 4. Just as inhibitors of the 5-HT uptake carrier can antagonize MDMA-induced [ H]5-HT release in vitro, coadministration of MDMA with an uptake inhibitor such as citalopram can completely block the acute depletion of 5-HT. Although citalopram also antagonized the MDMA-induced decrease in TPH activity, there was still a significant loss of enzyme activity when compared to control. This implies that if MDMA requires access to the interior of the nerve terminals to affect TPH activity, it does not require the activity of the uptake carrier to gain entrance. Hence, these results are consistent with the outcome of synaptosomal uptake experiments with [ HJMDMA (Schmidt et al. 1987), which show that MDMA is not actively concentrated by a carrier system. Furthermore, it is apparent that the loss of enzyme activity alone is not sufficient to reduce 5-HT concentrations, but that release via the carrier must occur simultaneously, to deplete the terminal once synthetic capacity is reduced. 

Gaddum, J.H. Drugs which antagonize the actions of 5-hydroxytryptamine on peripheral tissues. In Lewis, G.P.. ed. 5-Hydroxytryptamine. 

Consroe, P. Boren, J.L. and Hsu, C.H. Propranolol antagonizes phencyclidine-induced hyperactivity and stereotypy in rats. Pharmacology 24 96-104, 1982. 

El Ouriaghli F, Fujiwara H, Melenhorst JJ, Sconocchia G, Hensel N, Barrett AJ. Neutrophil elastase enzymatically antagonizes the in vitro action of G-CSF implications for the regulation of granulopoiesis. Blood 2003 101(5) 1752-1758. 

Here, KA and KB are the dissociation equilibrium constants for the binding of agonist and antagonist, respectively. This is the Gaddum equation, named after J. H. Gaddum, who was the first to derive it in the context of competitive antagonism. Note that if [B] is set to zero, we have the Hill-Langmuir equation (Section 1.2.1). 

This is the Schild equation, which was first stated and applied to the study of competitive antagonism by H. O. Schild in 1949. It is probably the most important single quantitative relationship in... 

Baghdoyan, H. A., Lydic, R., Callaway, C. W. Hobson, J. A. (1989). The carbachol-induced enhancement of desynchronized sleep signs is dose dependent and antagonized by centrally administered atropine. Neuropsychopharmacology 2, 67-79. 

Schilstrom, B., Nomikos, G.G., Nisell, M., Hertel, P., Svensson, T.H. A-Methyl-D-aspartate receptor antagonism in the ventral tegmental area diminishes the systemic nicotine-induced dopamine release in the nucleus accumbens. Neuroscience. 82 781, 1998. 

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