Comparison of the vasoconstrictor effects of the selective 5-HT1D -receptor agonist L-775,606 with the mixed 5-HT1B /1D -receptor agonist sumatriptan and 5-HT in human isolated coronary artery

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5-HT1D receptor agonists and human coronary artery reactivity in vitro: crossover comparisons of 5-HT and sumatriptan with rizatriptan and L-741,519.

1. Rizatriptan (MK-462, (N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl] ethylamine)) and its structurally related analogue L-741,519 (N-methyl-4-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]piperidine) are novel 5-HT1D-receptor agonists. Rizatriptan has shown efficacy as an anti-migraine agent in clinical trials. Since angiographic studies in patients have shown that sumatriptan (an estab...

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Mechanisms of action of the 5-HT1B/1D receptor agonists.

Recent studies of the pathophysiology of migraine provide evidence that the headache phase is associated with multiple physiologic actions. These actions include the release of vasoactive neuropeptides by the trigeminovascular system, vasodilation of intracranial extracerebral vessels, and increased nociceptive neurotransmission within the central trigeminocervical complex. The 5-HT(1B/1D) rece...

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Differential involvement of 5-HT1A and 5-HT1B/1D receptor in human interferon -induced immobility

Although Interferon-alpha (IFN-α) is a powerful drug in treating several viral infections and certain tumors, a considerable amount of neuropsychiatry side-effects such as depression and anxiety are unavoidable consequence. Combination with selective serotonin (5-HT) reuptake inhibitor (SSRI) fluoxetine significantly improved the situation. However, the potential 5-HT1A receptorand 5-HT1B recep...

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Effects of 5-HT1B/1D receptor agonist rizatriptan on cerebral blood flow and blood volume in normal circulation.

To investigate the vasoconstrictor effect of 5-hydroxytryptamine (5-HT1B/1D) receptor agonists for migraine treatment, changes in cerebral blood flow (CBF) and blood volume induced by rizatriptan were assessed by positron emission tomography (PET). Eleven healthy volunteers underwent PET studies before and after rizatriptan administration. Dynamic PET data were acquired after bolus injection of...

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ژورنال

عنوان ژورنال: British Journal of Clinical Pharmacology

سال: 2000

ISSN: 0306-5251

DOI: 10.1046/j.1365-2125.2000.00129.x