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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Change of 5-hydroxytryptamine (5-HT) concentrations in platelets from patients with chronic tension-type headache (TH) and controls were observed during cold pressor test (CPT). Before cold stimulation, 5-HT concentrations in platelets from patients with TH were significantly lower than those found in controls. One minute after the start of cold stimulation, 5-HT levels in platelets from patients with TH were significantly much lower than in the controls, as control levels rose and TH levels fell. The results show that, under stress, the absorbance of 5-HT into the platelets in patients with TH is reduced. It is suggested that, in patients with TH, there are abnormalities of 5-HT uptake into platelets and factors which cause release of 5-HT from platelets.
Headache 1990 Sep
PMID:Alteration of platelet serotonin in patients with chronic tension-type headache during cold pressor test. 226 11

This paper reports part of a study which investigated the identity of the receptor involved in 5-hydroxytryptamine (5-HT) mediated contraction of the human basilar artery in vitro. 5-HT and a variety of 5-HT receptor agonists contracted human isolated basilar artery with a rank order of agonist potency: 5-carboxamidotryptamine greater than 5-HT greater than GR43175 much much greater than 2-methyl-5-HT. The maximum response produced by these agonists differed. The contractile responses to both 5-HT and GR43175 were resistant to antagonism by the 5-HT2 antagonist ketanserin and the 5-HT3 antagonist GR38032, indicating that neither 5-HT nor GR43175 activate 5-HT2 and 5-HT3 receptors in this tissue. In striking contrast, methiothepin (an antagonist at 5-HT1-like receptors) proved a potent antagonist of the contractile actions of both 5-HT and GR43175. Methiothepin did not antagonize the contractile response to the thromboxane-A2 mimetic U-46619. It is concluded that 5-HT and GR43175 contract the human isolated basilar artery by activating 5-HT1-like receptors. It is suggested that the antimigraine action of GR43175 may reflect its ability to constrict certain cranial arteries via 5-HT1-like receptor activation.
Cephalalgia 1989
PMID:Characterization of the 5-hydroxytryptamine receptor which mediates contraction of the human isolated basilar artery. 254 83

The selective serotonin-1A receptor partial agonist anxiolytics represent a new class of pharmacologic agents that have demonstrated efficacy in the treatment of generalized anxiety disorder (GAD). These compounds offer a completely different pharmacologic approach to this disorder from previous medications. The selective 5-hydroxytryptamine-1A (5-HT1A) anxiolytics buspirone, gepirone, ipsapirone, and SM-3997 have several important new and unique features that will be reviewed in this paper. These features include no cross-tolerance with alcohol or benzodiazepines, no evidence of abuse or misuse potential, and no withdrawal symptoms or rebound anxiety on cessation of therapy. The 5-HT1A anxiolytics have no muscle relaxant, sedative, or anticonvulsant properties and do not impair psychomotor functioning. They do have a slower onset of effect than standard benzodiazepines-clinical response is usually noted in 1-3 weeks. The side effect profile is quite different from that of the benzodiazepines. It includes gastrointestinal symptoms such as nausea and diarrhea, headache, dizziness, and restlessness. Some patients with GAD who have received chronic (greater than 1 month) benzodiazepine therapy may not respond as well to these compounds initially as will patients with no prior benzodiazepine treatment, especially if the benzodiazepine has been discontinued only recently. These compounds, buspirone in particular, have been shown to have excellent maintenance and prophylactic properties and to be well tolerated with long-term therapy (greater than 3 months). Because of their unique mechanism of action and side effect profile, and no evidence of misuse or abuse potential or interference with mental acuity, these compounds represent a definite advance in the pharmacologic management of GAD.
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PMID:Serotonin-1A anxiolytics: an overview. 256 39

The action of ergotamine on the 5-hydroxytryptamine (5-HT) venous sensitivity was studied in ergotamine abuser and non-abuser migraine patients. Ergotamine abusers showed reduced 5-HT hand vein contraction during abuse, compared to seven days after ergotamine withdrawal. In non-ergotamine users, the 5-HT venoconstriction was not significantly modified 12 h after a single intramuscular ergotamine (0.25 mg) administration. Even the administration of ergotamine locally into the vein did not change the venospasm of 5-HT given acutely in the same vein. Therefore, it seems that the 5-HT antagonism does not contribute to the therapeutic effect of ergotamine during the migraine attack. Moreover, the reduced 5-HT responsiveness during ergotamine abuse may possibly be compatible with the chronic headache present in some abusers, the withdrawal headache attacks and the abuse itself.
Cephalalgia 1989 Dec
PMID:Reduced serotonin vascular sensitivity in ergotamine abusers. 261 83

The availability of selective compounds has made it possible to subdivide 5-hydroxytryptamine (5-HT) receptors into three distinct types, called 5-HT1-like, 5-HT2 and 5-HT3. The selective agonists at the three receptor types are, respectively, 5-carboxamidotryptamine, alpha-methyl-5-HT and 2-methyl-5-HT. While no selective antagonists are yet available for the 5-HT1-like receptors, some compounds, including ketanserin and MDL 72222, selectively antagonize 5-HT2 and 5-HT3 receptors respectively. Depending upon experimental conditions, 5-HT causes a constriction or dilatation of cerebral and extracerebral cranial vessels. Vascular contraction by 5-HT seems to be mediated primarily via 5-HT2 receptors (located mainly on large conducting vessels), though in several instances (for example, dog and human basilar arteries and porcine arteriovenous anastomoses; AVAs) 5-HT1-like receptors are involved in addition to or in place of 5-HT2 receptors. In the rabbit ear and external carotid arteries 5-HT may act directly on alpha-adrenoceptors. Arteriolar dilatation, leading to increased capillary ("nutrient") blood flow, occurs via 5-HT1-like receptors. However, the 5-HT1-like receptors on the arterioles and AVAs appear to be similar but not identical. Since a reduction of plasma 5-HT and opening of AVAs have been implicated in the pathophysiology of migraine, compounds acting on 5-HT1-like receptors to close the shunt vessels can be expected to have therapeutic activity in migraine.
Cephalalgia 1989
PMID:Characterization of 5-hydroxytryptamine receptors in the cranial vasculature. 266 Oct 12

Pipethiadene, a prophylactic of vasomotoric headaches of the series of 4,9-dihydrothieno(2,3-c)-2-benzothiepine derivatives, shows a peripheralpharmacological profile of an antiallergic agent. The experiments in rats showed a high antianaphylactic effect of pipethiadene in the passive cutaneous anaphylaxis (PCA) test. Pipethiadene also exerted intensive antianaphylactoid action in rats on the liberator of histamine, compound 48/80, on dextran, and in the use of a combination of ovalbumin with indomethacin. In comparative pharmacological experiments with pizotifen and cyproheptadine an attempt was made to estimate the relative role of histamine and 5-hydroxytryptamine 5-HT) mediators in the employed experimental procedures in rats.
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PMID:[Anti-allergic properties of pipethiaden--a new preventive agent for migraine]. 279 Sep 93

In migraine, the role of platelets is regarded as an important factor. We investigated plasma beta-thromboglobulin (BTG), platelet factor 4 (PF4), and 5-hydroxytryptamine (5-HT) in migraine patients and muscle contraction headache (MCH) patients during headache-free periods. The mean values of the plasma BTG, PF4, and 5-HT concentrations in the migraine group and the MCH group were significantly higher than those in healthy controls. The mean value of the plasma BTG concentration was significantly higher in the migraine group than in the MCH group, but the differences in the mean plasma PF4 and 5-HT concentrations between the two groups were not significant. Continuous platelet activation exists in both MCH patients and migraine patients. From the biochemical point of view, we have provided evidence for a similarity between migraine and MCH.
Cephalalgia 1987 Dec
PMID:Platelet activation in muscle contraction headache and migraine. 296 39

A recently developed method for analysing 5-hydroxytryptamine (5-HT) efflux from platelets preloaded with a small amount of 14C-5-HT enables the assessment of the relative size of the granular and the cytoplasmatic pools of 5-HT within the platelets and of the rate of spontaneous efflux from these two compartments. This method, together with conventional assessment of the 5-HT uptake measures Km and Vmax, was applied in this study, comparing platelets from 14 patients with common migraine and 10 patients with classic migraine with platelets from 25 healthy controls. All patients were unmedicated and in an attack-free period. Neither the total patient group nor either of the two subgroups differed significantly from the control group on any measure of 5-HT uptake or efflux. However, two differences approached the conventional significance level: the relative size of the granular compartment (Compartment III) was larger for classic than for common migraine, and the efflux rate from Compartment III was shorter for classic migraine than for the healthy controls (P approximately 0.10 in both cases). Further studies are required to show whether these differences are real and, if so, whether they have any relevance for the pathogenesis of migraine attacks.
Cephalalgia 1986 Sep
PMID:The uptake, storage, and efflux of serotonin in platelets from migraine patients. 376 47

Concentrations of 5-hydroxytryptamine (5-HT) in platelets were determined in 33 cluster headache patients (17 males) and in 34 migraine patients (16 males) outside attacks. The 5-HT uptake into platelets was measured and the kinetic constants Vmax and Km determined in 26 cluster patients (14 males) and in 30 migraine patients (13 males). Significantly lower 5-HT concentrations in whole blood were found in cluster headache and migraine patients than in 50 healthy controls (19 males). The Vmax and Km values of the 5-HT uptake were significantly lower in cluster headache and migraine patients compared with 22 healthy controls (9 males). The 5-HT concentrations and the kinetics of the 5-HT uptake did not differ between cluster headache and migraine. In healthy controls a significant positive correlation was found between the 5-HT uptake rate at 0.25 microM and Km but not in cluster headache and migraine patients. The 5-HT concentrations in whole blood correlated positively with Vmax and Km, respectively, in cluster headache and with Km in healthy controls but not with Vmax nor with Km in migraine. There was no obvious relation between the kinetics of platelet monoamine oxidase (MAO) and the 5-HT uptake except for an increased incidence of low Vmax of MAO and low Km of the 5-HT uptake in cluster headache. The kinetics of the 5-HT uptake was apparently not related to the state of migraine. The results indicate a possible constitutional trait in cluster headache and migraine expressed as low 5-HT concentrations in whole blood and low Vmax and Km of the 5-HT uptake into platelets.
Cephalalgia 1985 Mar
PMID:Concentration and uptake of 5-hydroxytryptamine in platelets from cluster headache and migraine patients. 392 Dec 57

Experiments were performed to assess the ability of bencianol (ZY15051) to reverse contractions of human basilar arteries in vitro that were induced by a wide range of substances implicated in the aetiology of migraine and cerebral arterial spasm. Bencianol caused a dose-related (1-100 micrograms ml-1) reversal of contractions induced by 5-hydroxytryptamine, noradrenaline, angiotensin II, prostaglandin F2 alpha, and U-46619 (a thromboxane-A2 mimetic). Bencianol was more effective against contractions induced by EC50 compared to maximal concentrations of each agent, and was least effective against the thromboxane-A2 mimetic, U-46619. In addition, contractions induced by thromboxane-A2-like substances generated from guinea-pig lungs were also reversed by bencianol but only at the highest concentration used (100 micrograms ml-1). The relevance of this action of bencianol to migraine and cerebral arterial spasm is discussed.
Cephalalgia 1985 Dec
PMID:Anti-spasmogenic effects of bencianol (ZY15051) on human cerebral arteries in vitro. 408 77


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