Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of eletriptan binding at human 5-HT1B and 5-HT1D receptors

Napier, Carolyn; Stewart, Michael; Melrose, Heather L.; Hopkins, Brian; McHarg, Aileen; Wallis, Rob

doi:10.1016/s0014-2999(99)00026-6

Cited by 72 publications

(57 citation statements)

References 35 publications

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“…3 The 5-HT 1B receptor is located on meningeal and coronary arteries, and its agonism produces vasoconstriction that is cranioselective. An analysis of vascular contraction of isolated middle meningeal artery, coronary artery, and saphenous vein in response to triptan administration showed concentration-dependent contraction that was selective for the middle meningeal artery relative to the other 2 blood vessels.…”

Section: Smentioning

confidence: 99%

“…The triptans are believed to exert their antimigraine effects via binding to 5-HT 1B/1D receptors on the trigeminal nerve and dural vasculature, where they act to reverse vasodilatation of blood vessels and also to reduce neurogenic inflammation. [1][2][3] Their lack of affinity at other receptors is the pharmacologic basis for the high degree of tolerability of triptans as a class. The safety and tolerability of triptans have been studied more extensively than other abortive therapies.…”

mentioning

confidence: 99%

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Evaluating the safety and tolerability profile of acute treatments for migraine

Martin

Goldstein

2005

The American Journal of Medicine Supplements

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Section: Smentioning

confidence: 99%

mentioning

confidence: 99%

Evaluating the safety and tolerability profile of acute treatments for migraine

Martin

Goldstein

2005

The American Journal of Medicine Supplements

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“…For example, aryl sulfones can be found in many marketed drugs used to treat migraines (2). The use of sulfones has become a classic strategy in the organic synthesis of many of the most demanding and sophisticated complex molecules (3).…”

Section: Introductionmentioning

confidence: 99%

S˭O homolytic bond dissociation enthalpies in sulfones: high-levelab initioand DFT study

Zheng

Chen

et al. 2012

Journal of Sulfur Chemistry

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2012) S˭O homolytic bond dissociation enthalpies in sulfones: high-level ab initio and DFT study, Journal of Sulfur Chemistry, 33:5, 541-559,The S=O bond dissociation enthalpies (BDE) of sulfone derivatives were calculated using high-level ab initio methods including G3, G3B3, CBS-Q, CBS-4M and MP2. Based on the comparison of these theoretical values and experimental ones, the performances of a number of density functional theory methods were then assessed. It was found that the KMLYP method gave the lowest root mean square error. We, therefore, used this method to calculate the S=O BDEs of a number of substituted sulfones. The electronic effect of the substituents and the remote substituent effect of aryl-substituted sulfones on S=O BDEs were investigated. In addition, a molecular orbital analysis of typical molecules was conducted in order to investigate the electronic effect on S=O BDEs. We also predicted several S=O BDE values of heteroaromatic-substituted sulfones using the KMLYP method.

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“…Morphine can apparently increase parasympathetic activity and suppress cardiovascular functions (Napier et al, 1999;Randich et al, 1991). Prolonged morphine administration and subsequent withdrawal can affect catecholamine turnover and thus myocardial adrenergic signaling and function (Chang and Dixon, 1990;Rabadan et al, 1997).…”

Section: Introductionmentioning

confidence: 99%

Morphine use in elderly patients with acute heart failure

Li¹

2012

Afr. J. Pharm. Pharmacol.

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Morphine has been considered as an important medicine to treat acute heart failure (AHF) for a long time. This study was designed to explore the usage rate of morphine in emergency department and its influence on the prognosis of the elderly patients with AHF in china. A prospective investigation of elderly patients with AHF, who were treated and admitted from emergency room of the General Hospital of the People's Liberation Army (GHPLA) in China, were performed. The patients were divided into two groups: control group and morphine treatment group. The relationships between the usage of morphine and clinical factors such as demographic characters of patients and past history were analyzed. The effect of morphine on mechanical ventilation, hospitalization stay and the mortality of patients were also evaluated. The usage rate of morphine was 50% in the emergency room. The patients on the morphine treatment group were more likely to have past history of coronary heart disease, type 2 diabetes mellitus (T2DM) and stroke than those of the control group (p < 0.05). The patients on morphine treatment group had higher troponin-T values compared with those of the control group (p < 0.05). Morphine usage was not an independent risk factor of mortality (OR: 2.172, p: 0.187, 95% CI: 0.686 to 6.879). The Odd ratio of morphine usage for mechanical ventilation incidence was 3.01 (95%CI, 1.22 to 7.41). High prevalence of morphine usage was found in the elderly AHF patients from emergency room of GHPLA in China. Morphine is still a safe medicine in early treatment on the elderly patients with AHF with mechanical ventilation in China.

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Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of eletriptan binding at human 5-HT1B and 5-HT1D receptors

Cited by 72 publications

References 35 publications

Evaluating the safety and tolerability profile of acute treatments for migraine

Evaluating the safety and tolerability profile of acute treatments for migraine

S˭O homolytic bond dissociation enthalpies in sulfones: high-levelab initioand DFT study

Morphine use in elderly patients with acute heart failure

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