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AT1 Receptor Antagonists

Current Medicinal Chemistry-Cardiovascular & Hematological Agents, 2004
Type 1 receptors (AT1) for the peptide hormone angiotensin II play a crucial role in the cardiovascular homeostasis. In this regard, several selective, orally active non-peptide antagonists have been developed for the treatment of hypertension and congestive heart failure.
I, Verheijen   +3 more
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Neurokinin receptor antagonists

Expert Opinion on Investigational Drugs, 2000
Studies on tachykinin peptides and the corresponding neurokinin receptors (NKr) have increased dramatically recently due to the discovery of selective, orally-active, metabolically stable and sometimes CNS penetrating NKr antagonists. After demonstrating the potential use for NKr antagonists in animal models, some compounds have recently progressed ...
V, Leroy, P, Mauser, Z, Gao, N P, Peet
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Prolactin Receptor Antagonists

Endocrine, 1998
Most prolactin (PRL) in the circulation is produced by the pituitary. However, a wide variety of traditional target tissues of the hormone have also been shown to produce their own prolactin. The amount produced per cell is low, but may well be sufficient for autocrine/paracrine activity.
C B, Kuo, D, Coss, A M, Walker
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Mineralocorticoid Receptor Antagonists

2019
Two mineralocorticoid receptor antagonists, spironolactone and eplerenone, are currently approved by the FDA. Several non-steroid based ligands are in clinical trials for indications including heart failure, hypertension and diabetic kidney disease, and even more structurally distinct chemical series are reported in the literature with preclinical data
Anneli, Nordqvist, Kenneth L, Granberg
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Orexin Receptor Antagonists

Pharmaceutical Patent Analyst, 2012
The orexin neuropeptides bind to two G protein-coupled receptors, orexin-1 and -2. Small-molecule antagonism of the receptors has potential therapeutic utility in a number of areas, most notably insomnia, for which the most advanced dual orexin receptor antagonist has now completed clinical trials.
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Vasopressin Receptor Antagonists

Current Hypertension Reports, 2015
Arginine vasopressin (AVP) is the principal hormone involved in regulating the tonicity of body fluids. Less appreciated is the role that AVP plays in a variety of other physiologic functions including glucose metabolism, cardiovascular homeostasis, bone metabolism, and cognitive behavior.
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Cholecystokinin receptor antagonists

American Journal of Physiology-Gastrointestinal and Liver Physiology, 1984
Since 1979 three classes of cholecystokinin receptor antagonists have been described: 1) derivatives of cyclic nucleotides, 2) derivatives of amino acids, and 3) C-terminal fragments or partial sequences of cholecystokinin. These various antagonists share a number of common features, such as their specific, reversible, and competitive actions, but ...
J D, Gardner, R T, Jensen
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Muscarinic Receptor Antagonists

2016
Parasympathetic activity is increased in patients with chronic obstructive pulmonary disease (COPD) and asthma and appears to be the major reversible component of airway obstruction. Therefore, treatment with muscarinic receptor antagonists is an effective bronchodilator therapy in COPD and also in asthmatic patients.
Maria Gabriella, Matera, Mario, Cazzola
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Mineralocorticoid receptor antagonists

Current Hypertension Reports, 2007
With an increasingly aging population, the need for effective treatment of cardiovascular diseases (eg, heart failure, hypertension, and ischemic heart disease) cannot be overemphasized. The vital importance of mineralocorticoid receptor antagonists for treating cardiovascular conditions has only been appreciated in the last decade. The re-emergence of
Parthasarathy, Hari Krishnan   +1 more
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Thrombin Receptor Antagonists

Seminars in Thrombosis and Hemostasis, 1996
Thrombin's proteolytically activated "tethered-ligand" receptor is widely expressed and mediates many of thrombin's actions on cells. Its central role in thrombin-stimulated human platelet activation and vascular smooth muscle proliferation as well as location in atherosclerotic plaques suggests receptor involvement in arterial thrombosis and ...
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