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Effects of 1-H-indole-3-glyoxamide (A-002) on concentration of secretory phospholipase A2 (PLASMA study): a phase II double-blind, randomised, placebo-controlled trial.

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BACKGROUND Secretory phospholipase A(2) (sPLA(2)) enzymes, produced and secreted in human blood vessels and hepatocytes, contribute to the development of atherosclerosis through mechanisms that are both dependent and independent of lipoprotein. We examined the effects of an sPLA(2) inhibitor on

SUMATRIPTAN: a receptor-targeted treatment for migraine.

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Sumatriptan, recently introduced for the treatment of migraine, heralds the beginning of a molecular era in the pharmacological treatment of migraine headache. An indole (non-ergot alkaloid) derivative with agonist properties at a receptor resembling the 5-HT1D subtype (so-called 5-HT1-like

Phase I/II study of the anti-oestrogen zindoxifene (D16726) in the treatment of advanced breast cancer. A Cancer Research Campaign Phase I/II Clinical Trials Committee study.

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We report a phase I/II study of the indole derivative, zindoxifene, an anti-oestrogen with intrinsic oestrogenic activity. We have treated 28 women with advanced breast cancer of whom 26 had received prior endocrine therapy. Oral zindoxifene doses ranged from 10 to 100 mg daily; doses were escalated

Pharmacokinetics and effect of food after oral administration of prolonged-release tablets of ropinirole hydrochloride in Japanese patients with Parkinson's disease.

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OBJECTIVE Ropinirole hydrochloride, a dopamine receptor agonist with a non-ergot alkaloid structure, is highly selective for the dopamine D(2) /D(3) receptors. This study was conducted to evaluate the steady-state pharmacokinetics, safety and efficacy after repeated oral administration of

5-HT3 antagonist ICS 205-930 enhances naltrexone's effects on ethanol intake.

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Opioid receptor antagonist naltrexone has shown some efficacy in decreasing ethanol consumption in humans. However, naltrexone treatment is not always efficacious and produces several aversive effects such as nausea, anxiety and weight loss. Serotonin-3 (5-HT3) receptor antagonists also modulate

Phase I trial of the thymidylate synthase inhibitor AG331 as a 5-day continuous infusion.

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AG331 (N6-[4-(morpholinosulfonyl)benzyl]-N6-methyl-2, 6-diaminobenz-[c,d]-indole glucuronate) is a lipophilic thymidylate synthase inhibitor with activity in solid tumor models. On the basis of preclinical data supporting regimens of frequent drug administration, we performed a Phase I trial of

Saw palmetto-induced pancreatitis.

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Saw palmetto is a frequently used botanical agent in benign prostatic enlargement (BPH). Although it has been reported to cause cholestatic hepatitis and many medical conditions, Saw palmetto has not been implicated in acute pancreatitis. We report a case of a probable Saw palmetto induced acute

Alniditan in the acute treatment of migraine attacks: a subcutaneous dose-finding study. Subcutaneous Alniditan Study Group.

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Alniditan is a new 5HT1D receptor agonist, belonging to a different chemical class from sumatriptan and other indole derivatives used or being developed for the treatment of acute migraine. In a multinational double-blind randomized parallel-groups dose-finding trial, alniditan was given

[Pharmacokinetics of azasetron (Serotone), a selective 5-HT3 receptor antagonist].

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5-HT3 receptor antagonists have been established in a number of clinical trials as effective agents in the management of nausea and vomiting induced by cancer chemotherapy including cisplatin. Azasetron (Serotone) is a potent and selective 5-HT3 receptor antagonist, and classified as benzamide

Acute poisoning due to non-steroidal anti-inflammatory drugs. Clinical features and management.

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Despite the widespread use of non-steroidal anti-inflammatory drugs (NSAIDs), the current number of reported cases of poisoning is small. However, with the introduction of 'over-the-counter' preparations of NSAIDs in some countries (e.g. ibuprofen in the UK and USA) an increased incidence of acute

A case of biliary carcinoid presenting with pancreatitis and obstructive jaundice.

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A 43-yr-old man presented to the clinic with abdominal pain, jaundice, nausea, and vomiting and weight loss over a 6-month period. Physical exam was unrevealing other than mild epigastric tenderness. A computed tomographic scan of the abdomen revealed a mass in the head of the pancreas, which was

Novel 5-hydroxytryptamine (5-HT3) receptor antagonists. II. Synthesis and structure-activity relationships of 4,5,6,7-tetrahydro-1H-benzimidazole derivatives.

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A novel series of 4,5,6,7-tetrahydro-1H-benzimidazole derivatives 4,5,6 and 7 was prepared and evaluated for activities as 5-hydroxytryptamine (5-HT3) receptor antagonists which may be useful for the treatment of irritable bowel syndrome (IBS) as well as nausea and vomiting associated with cancer

[Emergency treatment of migraine attacks with particular reference to agonists of 5-HT1B/1D receptor].

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The author discusses the modern methods of emergency controlling of migraine attacks, especially the recently introduced drugs agonists of the 5-HT 1B/1D receptor /Sumatriptan, Zolmitriptan/ and prophylactic treatment. In light and moderately severe attacks analgesics are usually effective as well

Abdominal vagi mediate c-Fos expression induced by X-ray irradiation in the nucleus tractus solitarii of the rat.

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The mechanism of induction of emesis by X-ray irradiation remains largely unknown. The purpose of the present research was to clarify the neuronal basis of the induction of nausea induced by X-ray irradiation analyzing c-Fos expression in the nucleus tractus solitarii (NTS) as a marker of cellular

[A new antiemetic ramosetron hydrochloride].

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Ramosetron hydrochloride as a 5-HT3 receptor antagonist-type antiemetic, which was developed in Japan. It has an indole ring which is the mother nucleus of serotonin (5-HT) and a tetrahydrobenzimidazol radical. These components are linked by a carbonyl radical. It was reported in non-clinical

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