Results 111 to 120 of about 169 (165)
Some of the next articles are maybe not open access.
Discovery of orally active prostaglandin D2 receptor antagonists
Bioorganic and Medicinal Chemistry Letters, 2004A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and evaluated for prostaglandin D(2) (DP) receptor affinity and antagonist activity. Some of them exhibited strong receptor binding and were potent in the cAMP formation assays.
Maki Iwahashi +2 more
exaly +3 more sources
Identification of an indole series of prostaglandin D2 receptor antagonists
Bioorganic and Medicinal Chemistry Letters, 2006A novel indole series of PGD2 receptor (DP receptor) antagonists is presented. Optimization of this series led to the identification of potent and selective DP receptor antagonists. In particular, antagonists 35 and 36 were identified with Ki values of 2.6 and 1.8 nM, respectively.
Nicolas Lachance +2 more
exaly +3 more sources
Quinacrine is a prostaglandin antagonist
Biochemical and Biophysical Research Communications, 1977Abstract Quinacrine, an anti-malarial with local anaesthetic properties, because of its fluorescence characteristics and its ability to combine with chromosomes and biological membranes has been widely used as a “probe”. The sites with which it combines in Torpedo marmorata electric organs have many of the characteristics of specific receptors.
D F, Horrobin +5 more
openaire +2 more sources
A Study of Prostaglandins and Prostaglandin Antagonists in Relation to Anaphylaxis in Calves
Canadian Journal of Physiology and Pharmacology, 1974Actions of prostaglandins (PG) E1, E2, and F2α on the cardiovascular–respiratory systems of anesthetized calves were studied in conjunction with the effects of a series of prostaglandin antagonists on acute systemic anaphylaxis. Meclofenamate, acetylsalicylic acid (ASA), phenylbutazone, and indomethacin, all inhibitors of PG synthesis, were ...
J F, Burka, P, Eyre
openaire +2 more sources
Pharmaceutical Patent Analyst, 2013
Prostaglandin antagonists, with their pharmacological effects, are well-known drugs capable of treating widely diffused illnesses, including pain and inflammation disorders. In recent years, a major research focus has been devoted to the identification of agents able to selectively antagonize each receptor with which prostaglandins interact.
Manuela, Borriello, Luigi Piero, Stasi
openaire +2 more sources
Prostaglandin antagonists, with their pharmacological effects, are well-known drugs capable of treating widely diffused illnesses, including pain and inflammation disorders. In recent years, a major research focus has been devoted to the identification of agents able to selectively antagonize each receptor with which prostaglandins interact.
Manuela, Borriello, Luigi Piero, Stasi
openaire +2 more sources
Antagonists of the Prostaglandin D2 Receptor CRTH2
Drug News & Perspectives, 2008Prostaglandin D(2) (PGD(2)) is produced by mast cells, Th2 lymphocytes and dendritic cells and causes activation of Th2 lymphocytes, eosinophils and basophils through a high-affinity interaction with the G protein-coupled receptor chemoattractant homologous receptor expressed on Th2 cells (CRTH2, also known as DP(2)).
Roy, Pettipher, Trevor T, Hansel
openaire +2 more sources
Amide and l-amino derivatives of F prostaglandins as prostaglandin antagonists
Nature, 1978THE formation in tissues and organs of the different prostaglandins (PGs) is now known to be associated with various pathophysiological situations. There is an urgent need for specific PG antagonists to facilitate experimental differentiation and analysis of the roles of these endogenous PGs.
Y T, Maddox +3 more
openaire +2 more sources
Studies of prostaglandins and prostaglandin antagonists on bovine pulmonary vein in vitro
Prostaglandins, 1974Abstract Acetylsalicylic acid (ASA), indomethacin, sodium meclofenamate (FEN), phenylbutazone (PB), phloretin phosphates (PP), SC-19220, and diethylcarbamazine citrate (DECC) were screened against histamine, 5-hydroxytryptamine (5-HT), bradykinin, acetylcholine, and prostaglandins (PG) E 1 , E 2 , and F 2α to determine their specificity in ...
J F, Burka, P, Eyre
openaire +2 more sources
Thrombosis Research, 1977
Abstract Platelet aggregation and secretion induced by PGG 2 and by analogues of PGH 2 and PGE 2 were inhibited by NO164. Inhibition was apparently competitive (K i ∼ 20 μM). Responses to ADP, vasopressin and arachidonic acid were unaffected. Inhibition of ADP-induced platelet aggregation by PGD 2 and PGE 2 (but not by PGE 1 ) was antagonised ...
D E, MacIntyre, J L, Gordon
openaire +2 more sources
Abstract Platelet aggregation and secretion induced by PGG 2 and by analogues of PGH 2 and PGE 2 were inhibited by NO164. Inhibition was apparently competitive (K i ∼ 20 μM). Responses to ADP, vasopressin and arachidonic acid were unaffected. Inhibition of ADP-induced platelet aggregation by PGD 2 and PGE 2 (but not by PGE 1 ) was antagonised ...
D E, MacIntyre, J L, Gordon
openaire +2 more sources
PROSTAGLANDINS AS ADRENERGIC ANTAGONISTS
Annals of the New York Academy of Sciences, 1967This paper briefly reviews the nature of prostaglandins and their biological activities emphasizing several examples in which there is an apparent antagonism between the actions of catecholamines and those of prostaglandins. Prostaglandins occur most frequently in reproductive tract tissues but are found in other tissues as well.
openaire +2 more sources