Vasopressin receptor antagonists [PDF]
The first non-peptide vasopressin receptor antagonist (VRA) was recently approved by the United States Food and Drug Administration, and several others are now in late stages of clinical development. Phase 3 trials indicate that these agents predictably reduce urine osmolality, increase electrolyte-free water excretion, and raise serum sodium ...
Arthur Greenberg, Joseph G. Verbalis
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Aldosterone receptor antagonists [PDF]
Blocking the mineralocorticoid receptor (MR) is one of the most effective ways of reducing blood pressure in patients with resistant hypertension and improving cardiovascular prognosis in patients with heart failure with reduced ejection fraction and left ventricular dysfunction after myocardial infarction.
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Leukotriene Receptor Antagonists [PDF]
In the past decade, heightened emphasis has been placed on the importance of inflammation in the pathogenesis of asthma. Although corticosteroids have remained the primary anti-inflammatory agents in the management of the persistent asthmatic, new classes of drugs have recently been added.
Nizar J. Jarjour, Marzena E. Krawiec
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Human interleukin-1 receptor antagonist is expressed in liver [PDF]
Using PCR and Northern blot analysis, an IL-1 receptor antagonist specific transcript was amplified from HepG2- and liver mRNA, cDNA clones coding for IL-1 receptor antagonist were isolated from a liver cDNA library and sequence comparison revealed ...
Estaller, C.+3 more
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Endothelin Receptors and Their Antagonists
All three members of the endothelin (ET) family of peptides, ET-1, ET-2, and ET-3, are expressed in the human kidney, with ET-1 being the predominant isoform. ET-1 and ET-2 bind to two G-protein-coupled receptors, ETA and ETB, whereas at physiological concentrations ET-3 has little affinity for the ET(A) receptor.
Maguire, Janet J, Davenport, Anthony P
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Kinin-B1 receptors in ischaemia-induced pancreatitis: Functional importance and cellular localisation [PDF]
In this study we compare the role of kininB1 and B2 receptors during ischaemia/reperfusion of rat pancreas. Our investigations were prompted by the observation that infusion of a kininB2 receptor antagonist produced significant improvement in acute ...
Ahluwalia A.+9 more
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Olfaction: Receptor Antagonistes [PDF]
Odor receptors of the mammalian olfactory system have long been known to be activated in combinatorial fashion by odorants. A large-scale study now reveals that inhibition of receptors by odorants is comparably prevalent and combinatorial.
Douglas Rioux, John R. Carlson
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Interaction of GABA and Excitatory Amino Acids in the Basolateral Amygdala: Role in Cardiovascular Regulation [PDF]
Activation of the amygdala in rats produces cardiovascular changes that include increases in heart rate and arterial pressure as well as behavioral changes characteristic of emotional arousal.
Cook, Jennifer C.+3 more
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Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands [PDF]
Short chain fatty acids (SCFAs) are produced in the gut by bacterial fermentation of poorly digested carbohydrates. A key mediator of their actions is the G protein-coupled Free Fatty Acid 2 (FFA2) receptor and this has been suggested as a therapeutic ...
Hansen, Anders Højgaard+6 more
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The Effects of Serotonin Receptor Antagonists on Contraction and Relaxation Responses Induced by Electrical Stimulation in the Rat Small Intestine [PDF]
Background: The main source of 5-HT in body is in enterchromafin cells of intestine, different studies mentioned different roles for endogenous 5-HT and receptors involved and it is not clearified the mechanism of action of endogenous 5-HT. Objectives:
Bianchi C+33 more
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