The pathogenesis of flushing attacks in patients with malignant carcinoid tumors is attributed to the direct pharmacologic effect of excessive amounts of circulating serotonin. It was hoped that potent serotonin antagonists might relieve symptoms of the carcinoid syndrome in the inoperable patient. The nature of flushing attacks was studied in carcinoid patients and the influence thereon of 3 s...

The pathogenesis of flushing attacks in patients with malignant carcinoid tumors is attributed to the direct pharmacologic effect of excessive amounts of circulating serotonin. It was hoped that potent serotonin antagonists might relieve symptoms of the carcinoid syndrome in the inoperable patient. The nature of flushing attacks was studied in carcinoid patients and the influence thereon of 3 s...

The folate antagonists, in particular amethoptenin (methotrexate), continue to be useful drugs for the treatment of certain neoplastic diseases in man. The effectiveness of amethoptenin in preventing DNA synthesis and cellular replication appears to be a consequence of inhibition of the enzyme dihydrofolate reductase. This premise is sup ported by in vivo studies which show that in patients tre...

For the last decades, anticoagulation for stroke prevention in atrial fibrillation (AF) as well as for the prophylaxis and long-term treatment of venous thromboembolism has been entirely based on vitamin K antagonists (VKA). Although very effective under optimal conditions, long-term treatment with these drugs is flawed by the fact that the time in the therapeutic range frequently is suboptimal...

The development of a new integrated approach to the generation of a novel type of insect neuropeptide (Np) antagonists and putative insect control agents based on backbone cyclic compounds is described. The approach, termed the backbone cyclic neuropeptide-based antagonist (BBC-NBA), was applied to the insect pyrokinin (PK)/pheromone biosynthesis activating neuropeptide (PBAN) family as a model...

Vanilloid receptor 1 (TRPV1) is activated by chemical ligands (e.g., capsaicin and protons) and heat. In this study, we show that (2E)-3-[2-piperidin-1-yl-6-(trifluoromethyl)pyridin-3-yl]-N-quinolin-7-ylacrylamide (AMG6880), 5-chloro-6-[(3R)-3-methyl-4-[6-(trifluoromethyl)-4-(3,4,5-trifluorophenyl)-1H-benzimidazol-2-yl]piperazin-1-yl]pyridin-3-yl)methanol (AMG7472), and N-(4-tertiarybutylphenyl...

BACKGROUND AND PURPOSE Calcium antagonists play an important role in clinical practice. However, most of them have serious side effects. We have synthesized a series of novel calcium antagonists, quaternary ammonium salt derivatives of haloperidol with N-p-methoxybenzyl (X1), N-m-methoxybenzyl (X2) and N-o-methoxybenzyl (X3) groups. The objective of this study was to investigate the bioactivity...

The role of GP IIb/IIIa antagonists has been focused on patients with acute coronary syndromes undergoing PCI. In the ISAR-REACT 2 study abciximab given in patients with NSTEACS undergoing PCI already treated with 600 mg clopidogrel improved 30-day death and reinfarction rate in troponin positive patients. In the large EARLY-ACS trial upstream therapy with eptifibatide in high risk with NSTE-AC...