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Journal of Molecular and Cellular Cardiology, 1986
In contrast to nifedipine-like calcium antagonists, calcium agonistic 1,4-dihydropyridines have vasoconstricting and positive inotropic properties. BAY K 8644 has become the prototype of this new class. Its enantiomers show opposite effects on the calcium channel: one acts as a calcium agonist with the pharmacological profile of the racemic compound ...
M, Bechem, M, Schramm
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In contrast to nifedipine-like calcium antagonists, calcium agonistic 1,4-dihydropyridines have vasoconstricting and positive inotropic properties. BAY K 8644 has become the prototype of this new class. Its enantiomers show opposite effects on the calcium channel: one acts as a calcium agonist with the pharmacological profile of the racemic compound ...
M, Bechem, M, Schramm
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Seminars in Neurology, 2001
Dopamine agonists provide an effective means of treating early, middle, and late stages of Parkinson's disease. This article outlines the advantages and disadvantages of dopamine agonists as compared with levodopa therapy. The features and costs of the four Food and Drug Administration-approved agonists (bromocriptine, pergolide, pramipexole, and ...
P, Tuite, B, Ebbitt
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Dopamine agonists provide an effective means of treating early, middle, and late stages of Parkinson's disease. This article outlines the advantages and disadvantages of dopamine agonists as compared with levodopa therapy. The features and costs of the four Food and Drug Administration-approved agonists (bromocriptine, pergolide, pramipexole, and ...
P, Tuite, B, Ebbitt
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Cellular and Molecular Neurobiology, 2019
Trace amine-associated receptors (TAARs) are a family of G protein-coupled receptors (GPCRs) that are evolutionarily conserved in vertebrates. The first discovered TAAR1 is mainly expressed in the brain, and is able to detect low abundant trace amines.
Zhengrong Xu, Qian Li
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Trace amine-associated receptors (TAARs) are a family of G protein-coupled receptors (GPCRs) that are evolutionarily conserved in vertebrates. The first discovered TAAR1 is mainly expressed in the brain, and is able to detect low abundant trace amines.
Zhengrong Xu, Qian Li
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A2A adenosine receptor agonists, antagonists, inverse agonists and partial agonists
2023The Gs-coupled A2A adenosine receptor (A2AAR) has been explored extensively as a pharmaceutical target, which has led to numerous clinical trials. However, only one selective A2AAR agonist (regadenoson, Lexiscan) and one selective A2AAR antagonist (istradefylline, Nouriast) have been approved by the FDA, as a pharmacological agent for myocardial ...
Kenneth A, Jacobson +2 more
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Agonists, partial agonists, antagonists, inverse agonists and agonist/antagonists?
Trends in Pharmacological Sciences, 1987The label placed on a drug influences its ultimate use. But interpretation ofin-vivo data has complicated the simple receptor theory of agonists and antagonists for certain classes of drugs.Terry Kenakin argues that clarification of such data — described in an extremely complex system — at a molecular level, will either obviate the need for terms such ...
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Progress in Neuro-Psychopharmacology and Biological Psychiatry, 1984
The efficacy of coupling between the benzodiazepine receptor and chloride channel as well as the coupling to the GABA receptor is differentially affected by different benzodiazepine ligands. In general, the order of efficacy with regard to allosteric effects of benzodiazepine ligands on the chloride channel ([35S]TBPS) and GABA receptor ([3H]muscimol),
P L, Wood +3 more
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The efficacy of coupling between the benzodiazepine receptor and chloride channel as well as the coupling to the GABA receptor is differentially affected by different benzodiazepine ligands. In general, the order of efficacy with regard to allosteric effects of benzodiazepine ligands on the chloride channel ([35S]TBPS) and GABA receptor ([3H]muscimol),
P L, Wood +3 more
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Clinical Obstetrics and Gynecology, 1989
The development of GnRH agonists has had a major impact on the practice of gynecology and reproductive endocrinology. The clinical usefulness of GnRH agonists will increase as modes of administration are improved and indications become better defined. GnRH agonists and, potentially, antagonists will provide a prompt, effective, and reversible method of
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The development of GnRH agonists has had a major impact on the practice of gynecology and reproductive endocrinology. The clinical usefulness of GnRH agonists will increase as modes of administration are improved and indications become better defined. GnRH agonists and, potentially, antagonists will provide a prompt, effective, and reversible method of
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Medical Clinics of North America, 1999
Dopamine agonists have been used in the treatment of Parkinson's disease (PD) since the mid 1970s. With the approval of two new agents in 1997, the number available in the United States is up to four; bromocriptine, pergolide, pramipexole, ropinirole.
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Dopamine agonists have been used in the treatment of Parkinson's disease (PD) since the mid 1970s. With the approval of two new agents in 1997, the number available in the United States is up to four; bromocriptine, pergolide, pramipexole, ropinirole.
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Annals of Internal Medicine, 1996
Considerable evidence links elevated blood cholesterol levels to the development of atherosclerosis. The National Cholesterol Education Program (NCEP) has recently published revised guidelines for detecting and treating hypercholesterolemia in adults.
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Considerable evidence links elevated blood cholesterol levels to the development of atherosclerosis. The National Cholesterol Education Program (NCEP) has recently published revised guidelines for detecting and treating hypercholesterolemia in adults.
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