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PubMed2001

Long-term efficacy and safety of oral almotriptan: interim analysis of a 1-year open study.

OBJECTIVE: To assess the long-term tolerability and safety of a single, oral 12.5-mg dose of almotriptan and its efficacy in alleviating pain associated with consecutive migraine episodes occurring during a 12-month period. BACKGROUND: While sumatriptan appears to be effective for treatment of migraine, the drug has several properties that limit its use. Almotriptan, a new selective 5-HT1B/1D agonist, may be better tolerated over the long term. METHODS: This 1-year study was conducted on 806 adults between the ages of 18 and 65 years suffering from migraine, either with or without aura. The patients met the criteria for study as outlined by the International Headache Society and were instructed on drug use. Oral almotriptan 12.5 mg was used to treat the attack of any pain severity and a second dose was permitted in case of relapse of pain during the first 24 hours. Rescue medication was provided. Efficacy and tolerability were assessed by a combination of patient reporting and clinical visit evaluations. RESULTS: Overall, almotriptan was well tolerated. At 2 hours, 81% of attacks were relieved; 56% of the subjects were entirely free of pain. These efficacy data are similar for the first as well as the last attack studied. At analysis, 534 patients had treated their migraines for at least 6 months. About half of all patients experienced at least one adverse event, with 87% of the events being mild or moderate in nature. The most frequent adverse events were back pain (7.23% of patients), bronchitis (5.76%), and influenzalike symptoms (5.62%). Seventy-one percent of the adverse events were not related to almotriptan use. CONCLUSIONS: Almotriptan at an oral dose of 12.5 mg is safe antimigraine treatment. The safety profile results are similar to those obtained in other controlled triptan clinical studies. Almotriptan is efficacious in moderate-to-severe migraine pain and can be used repeatedly in recurrent episodes. The long-term safety data will be reanalyzed when full data become available.

Adult↗
PubMed2001

Successful use of propranolol in migraine associated with electroconvulsive therapy.

To date, there have been no reports on the use of propranolol in electroconvulsive therapy (ECT)-induced migraine; we describe a 32-year-old woman who was successfully treated with propranolol for this condition. Over a course of ECT, the patient developed increasingly severe migraine which was refractory to treatment with acetaminophen, codeine, and naproxen. Sumatriptan did not relieve the headache and aggravated the nausea. Successful migraine relief was achieved with a combination of propranolol and naproxen, administered before and after ECT. Propranolol reduced blood pressure and decreased the heart rate, measured before and immediately after ECT. Propranolol, possibly in combination with naproxen, may be useful in both acute and prophylactic treatment of post-ECT migraine.

Adult↗
PubMed2001

Naratriptan as short-term prophylaxis of menstrually associated migraine: a randomized, double-blind, placebo-controlled study.

OBJECTIVE: To determine the efficacy of naratriptan 1-mg and 2.5-mg tablets twice daily compared with placebo as short-term prophylaxis of menstrually associated migraine. BACKGROUND: Approximately 60% of women with migraine report headaches associated with their menstrual cycles. Results from an open-label study suggest that short-term administration of sumatriptan is useful in the prophylaxis of menstrually associated migraine. METHODS: A randomized, double-blind, three-arm, parallel-group, placebo-controlled study was conducted in women aged 18 years or older with a history of migraine with or without aura, as defined by the International Headache Society, of at least 6 months. Two dose strengths of naratriptan (1 mg, 2.5 mg) or identical-appearing placebo tablets (1:1:1) were administered twice daily for 5 days starting 2 days prior to the expected onset of menses across four perimenstrual periods. End points included the number of menstrually associated migraines, total migraine days, peak headache severity, lost work/activity time, migraine-related quality of life, and incidence of adverse events. RESULTS: Overall, the intent-to-treat population comprised 206 women (naratriptan 1 mg, n = 70; naratriptan 2.5 mg, n = 70, and placebo, n = 66); 171 women treated four perimenstrual periods. Significantly more perimenstrual periods per subject treated with naratriptan, 1 mg, were headache-free compared with placebo (50% versus 25%, P =.003). Naratriptan, 1 mg, significantly reduced the number of menstrually associated migraines (2.0 versus 4.0, P <.05) and menstrually associated migraine days (4.2 versus 7.0, P <.01) compared with placebo. More patients treated with naratriptan, 1 mg, were headache-free across all treated perimenstrual periods compared with placebo (23% versus 8%). No difference in headache severity was observed in breakthrough headaches. The incidence and severity of adverse events was similar across treatment groups. Naratriptan, 2.5 mg, was not statistically superior to placebo for any measure. CONCLUSIONS: Naratriptan, 1 mg, with tolerability similar to placebo, is an effective, short-term, prophylactic treatment for menstrually associated migraine.

Adult↗
PubMed2002

Frovatriptan for the acute treatment of migraine: a dose-finding study.

OBJECTIVE: To determine the optimal dose and tolerability of frovatriptan in the acute treatment of migraine. BACKGROUND: Frovatriptan has a distinctive pharmacological and pharmacokinetic profile compared with sumatriptan. A previous study has shown that frovatriptan doses of 2.5, 5, 10, 20, and 40 mg are equally effective in relieving headache with no evidence of a dose-response relationship. The incidence of adverse events tended to increase with doses of 10 mg and above. METHODS: This study was a randomized, double-blind, placebo-controlled, parallel-group multicenter trial. Patients (n=635) took a single oral dose of placebo or frovatriptan, 0.5, 1, 2.5, or 5 mg, at the onset of a moderate or severe migraine headache and recorded headache intensity, functional impairment, and migraine-associated symptoms over 24 hours. RESULTS: Frovatriptan 2.5 mg produced clinically and statistically significant headache relief 2 hours post-dose, whereas the effect of lower doses was not significantly different from that of placebo at that time point. The 2.5-mg dose also produced significant symptom relief and improvement in functional impairment. All doses of frovatriptan were well tolerated, and the majority of adverse events were of mild or moderate severity. CONCLUSION: It is concluded that the 2.5-mg dose of frovatriptan offers optimal efficacy and tolerability in the treatment of acute migraine. Higher doses do not appear to confer greater efficacy and are associated with an increased incidence of adverse effects.

Administration, Oral↗
PubMed2002

Naratriptan in the prophylaxis of cluster headache.

A 36-year-old man with cluster headache refractory to trials of standard prophylactic treatment and only partially responsive to parenteral sumatriptan and inhaled oxygen was admitted to an inpatient pain unit. The diagnosis of cluster headache was confirmed by direct observation of a typical attack. Despite efforts at prophylaxis, the patient continued to experience three to four severe headaches per day. Attempts to control his headaches with scheduled parenteral dihydroergotamine were successful, but headaches recurred when the medication was tapered, and continuous or intermittent use of parenteral dihydroergotamine was not felt to be a practical option for the patient. Naratriptan 2.5 mg twice daily completely abolished his headaches, which recurred when the medication was discontinued. No electrocardiographic or laboratory abnormalities were observed during treatment, and the patient reported no side effects.

Adult↗
PubMed2003

Coprescription of triptans with potentially interacting medications: a cohort study involving 240,268 patients.

BACKGROUND: Little information exists about the actual prescription of triptans within large, geographically diverse populations, in terms of demographic characteristics and co-prescriptions with other medications with potential interactions. OBJECTIVES: To investigate the demographic characteristics associated with triptan use, and examine the rate of co-prescription of triptans with specified pharmacologic agents with the potential for drug interactions. METHODS: This study examined the rate of co-prescription of triptans available in the US up to May 2001 (sumatriptan, naratriptan, rizatriptan, and zolmitriptan) with specified agents with potential for drug interactions. A cohort of 240,268 patients receiving pharmacy benefits from Merck-Medco (N = 65 + M) was followed over a one-year period. This analysis included patients who received at least two triptan prescriptions during the study (6/00-5/01). Ninety-one percent of the cohort remained on the same triptan during the study period. 'Co-prescription' was defined as any fill for a medication that was contraindicated or could potentially adversely interact with a triptan, obtained between and during the first and last triptan fills throughout the study period. RESULTS: Mean patient age was 43 (SD +/- 11.6) and 82% were female. Twenty-one percent were co-prescribed selective serotonin reuptake inhibitors, reflecting the considerable co-morbidity of migraine and depression. Patients taking triptans were almost never co-prescribed monoamine oxidase inhibitors (0.02%), and co-prescription of ergots was also low (1.45%). Less than one percent (0.45%) received cimetidine while taking zolmitriptan, while 2.7% of patients taking rizatriptan 10 mg also took propranolol. While agents unavailable in the U.S. were not evaluated in this cohort, six percent of patients were treated with potent CYP 3A4 inhibitors, which would not be expected to cause any problems with the triptans in the survey. However, such agents are specifically contraindicated for use with one triptan (eletriptan), recently launched in the EU, suggesting that continued vigilance will be necessary to avoid coprescription of medicines with the potential for producing adverse side effects. CONCLUSIONS: Triptan use mirrors migraine demographics. The frequency of co-prescription of triptans with SSRIs is about 20%. Continued vigilance will be necessary to avoid co-prescription of medicines with the potential for producing adverse drug events.

Adolescent↗
PubMed2003

Health care utilization in patients with migraine: demographics and patterns of care in the ambulatory setting.

BACKGROUND: Migraine affects people of all races and both sexes. Migraineurs suffer both financial losses and impaired quality of life. Recent progress in the treatment of migraine has not been made readily available to all who suffer the condition. OBJECTIVE: To assess outpatient health care delivery patterns for migraine sufferers in the United States. METHODS: National Ambulatory Medical Care Survey data from 1990 to 1998 was used to assess the demographics of patients seen with a diagnosis of migraine, the types of physicians they saw, and the medications used to treat migraine. RESULTS: Women accounted for 79% of visits for migraines and whites for 91% of the visits. There was a dramatic increase in the number of migraine visits during the study period, from 9.4 visits per 1000 people in 1990 to 18 visits per 1000 in 1998. Primary care physicians saw the majority of patients (72.2%). Butalbital/aspirin/caffeine was the drug most commonly prescribed for migraine treatment, followed by acetaminophen/dichloralphenazone/isometheptene mucate, propranolol, and sumatriptan. CONCLUSION: Perhaps in part due to newer treatment options, the number of visits for the treatment of migraine doubled over the study interval. Even so, most patients with migraine continue to be treated with older and presumably less effective medications.

Adolescent↗
PubMed2003

Demographic and migraine characteristics of adolescents with migraine: Glaxo Wellcome clinical trials' database.

OBJECTIVE: To describe the demographics and migraine characteristics of patients in the Glaxo Wellcome adolescent clinical trials' database. METHODS: Data from 8 sumatriptan (tablet and nasal spray) and naratriptan (tablet) trials (6 placebo controlled and 2 open label) were reviewed. Adolescents aged 12 to 17 years who had participated in migraine clinical trials and used at least 1 dose of study medication were summarized using descriptive statistics. Patient demographic (gender, age, race, height, and weight) and migraine (diagnosis, pain location and intensity, time and day of migraine onset and treatment, and associated symptoms) characteristics were examined. RESULTS: One thousand nine hundred thirty-two adolescents with migraine were identified; mean age was 14.1 years (standard deviation, 1.64; range, 11 to 18) and 54% of patients were female. More males were represented in the 12- to 14-year-old group (646 [73%] of 885) than in the 15- to 17-year-old group (234 [26%] of 885). Most patients reported migraine without aura (67%, 1121 of 1672), unilateral migraine pain (58%, 458 of 787), and pulsating pain (74%, 582 of 790). Migraine was aggravated by physical activity in most of the adolescents (88%, 526 of 598). Most migraine attacks (73%, 1363 of 1858) began between 6 am and 6 pm, and proportionately more attacks occurred Monday through Wednesday. Pretreatment vomiting was experienced by 5% (97 of 1830) of patients, nausea by 53% (983 of 1849), and photophobia or phonophobia (or both) by 88% (1628 of 1858) of patients. The incidence of associated symptoms was directly related to pretreatment headache severity. CONCLUSIONS: In this large clinical trials' database, adolescents had migraine without aura characterized by unilateral and pulsating pain and aggravated by activity. The incidence of associated symptoms was directly related to pretreatment pain intensity. More migraines occurred Monday through Wednesday during typical school hours. These data may facilitate clinicians' efforts to tailor migraine therapy to the needs of this patient population.

Adolescent↗
PubMed2000

Acute abstinence syndrome following abrupt cessation of long-term use of tramadol (Ultram): a case study.

We report on a patient who had taken the centrally acting analgesic tramadol for over 1 year. The compound had proven to be sufficient to treat her painful episodes related to fibromyalgia. Due to lack of supply while being on a trip, intake of the drug was stopped abruptly, resulting in the development of classical abstinence-like symptoms within 1 week. Abstinence-like symptoms consisted of restlessness and insomnia for which the benzodiazepine lorazepam was given. Diarrhoea and abdominal cramps were treated with the peripherally active opioid loperamide, while bouts of cephalgia were treated with sumatriptan. Diffuse musculoskeletal-related pain and restless leg syndrome (RLS) were treated with dextromethorphan. All these different medications proved to be efficacious as they resulted in the cessation of symptoms. Within 1 week symptoms ceased and the patient regained her normal activities without any sequelae. Although tramadol is considered a non-habit- and non-dependence-forming analgesic, abstinence symptoms are likely to develop following abrupt cessation of intake, especially when the compound had been taken over 1 year. Therefore patients should be advised of such an effect whenever they decide to stop intake or their physician is planning to switch to another medication. To avoid abstinence-like symptoms doses should be slowly tapered down.

Acute Disease↗
PubMed2001

An audit of accidental dural puncture during epidural insertion of a Tuohy needle in obstetric patients.

We report a prospective audit of 100 parturients who experienced accidental dural puncture by a Tuohy needle, while attending a tertiary referral obstetric unit during the period 1993-1999. The post dural puncture headache rate was 81% and the diagnosis of dural puncture was delayed until presentation of the headache in 27% of these cases. The incidence of unrecognised dural puncture was not influenced by the technique used for identification of the epidural space. Intraspinal opioid administration after dural puncture was associated with a significant reduction in the incidence of headache (P < 0.04). There was no association between mode of delivery and post dural puncture headache. Deliberate cannulation of the subarachnoid space with an epidural catheter at the time of dural puncture, for continuous spinal analgesia or anaesthesia, did not affect the incidence of post dural puncture headache but was associated with a significantly reduced rate of epidural blood patch (43% versus 80%, P < 0.01). Of those who developed post dural puncture headache, 48% were classified 'severe' and in 49% the headache presented within 24 h of dural puncture. There was a trend to earlier onset of headache (either immediate or within 24 h) when the epidural identification technique was loss-of-resistance to air rather than saline (54% versus 33%, P = 0.07). Twenty-eight percent of those suffering from post dural puncture headache were treated expectantly and 72% received a therapeutic blood patch. Of seven parturients who received sumatriptan, six found it ineffective and five subsequently received a blood patch.

Journal Article↗
PubMed2005

[Extrahepatic cholestasia during therapy with Zolmitriptan (AscoTop)].

Because of recurrent abdominal pain, jaundice and elevated liver function tests, a sixty-two-year old man had been referred to hospital several times within the preceding six months. By means of ultrasonography, endoscopic retrograde cholangiopancreatography (ERCP) and magnetic resonant cholangiopancreatography, dilated extrahepatic bile ducts were diagnosed. Stones and a tumorous process were excluded. ERCP showed hypermotility of the upper gastrointestinal tract. Quantitative hepatobiliary scintigraphy demonstrated retention of activity in the intra- and extrahepatic bile ducts and delayed transit of activity to the duodenum as signs of papillary dysfunction. Drug anamnesis revealed that the patient had started migraine treatment with Zolmitiptan, a 5-HT (1B/1D)-receptor agonist of the second generation, six months before the beginning of the cholestasia syndrome. Because of the known increase in amplitudes of oesophageal motor waves and of lower oesophageal sphincter tone by Sumatriptan, a 5-HT (1B/1D)-receptor agonist of the first generation, Zolmitriptan treatment was stopped. Thereupon, laboratory findings normalised and the patient has been feeling well for more than one year. Serotonin is an important monamine neurotransmitter that acts both in the CNS and in the gastrointestinal tract on identical receptors and is transported by the same systems. Thus it is not surprising that therapeutic measures which influence the serotoninergic system in the CNS are also effective in the enteric nervous.

Bile Ducts, Extrahepatic↗
PubMed2006

Diagnosis and treatment of cluster headache.

Cluster headache is an uncommon yet distinctive neurovascular syndrome occurring in either episodic or chronic patterns. The most unique feature of cluster headache is the unmistakable circadian and circannual periodicity. The attacks are stereotypical, that is, of extreme intensity, of short duration, occurring unilaterally, and associated with robust signs and symptoms of autonomic dysfunction. Unlike migraine, during an attack the patient with cluster headache often paces about. Attacks frequently occur at night, awakening the patient from sleep. Although the pathophysiology of cluster headache remains to be fully elucidated, several seminal observations have recently been made. The medical treatment of cluster headache includes acute, transitional, and maintenance prophylaxis. Agents used for acute therapy include inhalation of oxygen and triptans, such as sumatriptan, and dihydroergotamine. Transitional prophylaxis refers to the short-term use of fast-acting agents. This typically involves either corticosteroids or ergotamine derivatives. The mainstay of prophylactic therapy is verapamil. Lithium, divalproex sodium, or topiramate may also be useful. As the sophistication of functional neuroimaging increases, so too will our ability to better understand the anatomic and metabolic perturbations that underlie cluster headache.

Cluster Headache↗
PubMed1997

Migraine treatment.

Migraine is a primary headache disorder characterized by recurring attacks of pain and associated symptoms. Migraine sufferers require a continuum of clinical care that depends on their disability and response to treatment. Treatment consists of: (1) prevention of attacks by avoidance of triggers; (2) the use of nonpharmacologic treatments; (3) treatment of the acute attack; and (4) long-term prophylactic therapy. Migraine is comorbid for affective disorders, epilepsy, stroke, and mitral valve prolapse. The therapy selected depends on the headache severity and frequency, the pattern of associated symptoms, comorbid illnesses, and the patient's treatment response profile. Acute treatment can be symptomatic or specific, using drugs such as dihydroergotamine (DHE) or sumatriptan. Preventive treatment can be episodic, subacute, or chronic. The major drug groups include beta-adrenergic blockers, anti-depressants, calcium channel blockers, serotonin antagonists, anticonvulsants, and nonsteroidal anti-inflammatory drugs (NSAIDs). These can be divided into two major categories and second-line choices.

Analgesics↗
PubMed1992

A human serotonin 1D receptor variant (5HT1D beta) encoded by an intronless gene on chromosome 6.

An intronless gene encoding a serotonin receptor (5HT1D beta) has been cloned and functionally expressed in mammalian fibroblast cultures. Based on the deduced amino acid sequence, the gene encodes a 390-amino acid protein displaying considerable homology, within putative transmembrane domains (approximately 75% identity) to the canine and human 5HT1D receptors. Membranes prepared from CHO cells stably expressing the receptor bound [3H]serotonin with high affinity (Kd 4 nM) and displayed a pharmacological profile consistent, but not identical, with that of the characterized serotonin 5HT1D receptor. Most notably, metergoline and serotonergic piperazine derivatives, as a group, display 3- to 8-fold lower affinity for the 5HT1D beta receptor than for the 5HT1D receptor, whereas both receptors display similar affinities for tryptamine derivatives, including the antimigraine drug sumatriptan. Northern blot analysis revealed an mRNA of approximately 5.5 kilobases expressed in human and monkey frontal cortex, medulla, striatum, hippocampus and amygdala but not in cerebellum, olfactory tubercle, and pituitary. The 5HT1D beta gene maps to human chromosome 6. The existence of multiple neuronal 5HT1D-like receptors may help account for some of the complexities associated with [3H]serotonin binding patterns in native membranes.

Amino Acid Sequence↗
PubMed1992

Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.

The serotonin 1D (5-HT1D) receptor is a pharmacologically defined binding site and functional receptor site. Observed variations in the properties of 5-HT1D receptors in different tissues have led to the speculation that multiple receptor proteins with slightly different properties may exist. We report here the cloning, deduced amino acid sequences, pharmacological properties, and second-messenger coupling of a pair of human 5-HT1D receptor genes, which we have designated 5-HT1D alpha and 5-HT1D beta due to their strong similarities in sequence, pharmacological properties, and second-messenger coupling. Both genes are free of introns in their coding regions, are expressed in the human cerebral cortex, and can couple to inhibition of adenylate cyclase activity. The pharmacological binding properties of these two human receptors are very similar, and match closely the pharmacological properties of human, bovine, and guinea pig 5-HT1D sites. Both receptors exhibit high-affinity binding of sumatriptan, a new anti-migraine medication, and thus are candidates for the pharmacological site of action of this drug.

Amino Acid Sequence↗
PubMed1993

Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.

Sequential polymerase chain reaction experiments were performed to amplify a unique sequence representing a guanine nucleotide-binding protein (G-protein)-coupled receptor from rat hypothalamic cDNA. Degenerate oligonucleotides corresponding to conserved amino acids from transmembrane domains III, V, and VI of known receptors [5-HT1A, 5-HT1C, and 5-HT2; 5-HT is serotonin (5-hydroxytryptamine)] were used as primers for the sequential reactions. The resulting product was subcloned and used to screen a rat genomic library to identify a full-length clone (MR77) containing an intronless open reading frame encoding a 366-amino acid seven-transmembrane domain protein. The human homolog was isolated, and its encoded protein had 93% overall amino acid identity with the rat sequence. Within the conserved transmembrane domains, the sequences exhibit approximately 52%, 59%, 65%, and 68% amino acid identity with the known rat 5-HT1A, rat 5-HT1B, rat 5-HT1D, and human 5-HT1E receptors, respectively. MR77 was subcloned into a eukaryotic expression vector system and expressed in CosM6 cells. Studies on broken cell preparations indicate that the expressed receptor exhibits 125I-labeled d-lysergic acid diethylamide (LSD) binding that can be displaced by serotonin but not by other biogenic amines. The specific binding is displaced by the selective 5-HT1D agonist sumatriptan but not by the mixed 5-HT1A/1D agonist 5-carboxyamidotryptamine. 125I-labeled LSD binding was competitively antagonized by the ergot alkaloids methysergide and ergotamine. HeLa cells transfected with the MR77 gene exhibited inhibition of adenylate cyclase in response to serotonin. MR77 is expressed at low levels throughout the brain, with the greatest expression in the cortex, hippocampus, and striatum. MR77 thus represents a 5-HT receptor of the 5-HT1 class, and we propose that, based on the pharmacological characterization, MR77 represents an additional 5-HT1E-like receptor.

Amino Acid Sequence↗
PubMed1993

Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain.

We report two serotonin (5-hydroxytryptamine, 5-HT) receptors, MR22 and REC17, that belong to the G-protein-associated receptor superfamily. MR22 and REC17 are 371 and 357 amino acids long, respectively, as deduced from nucleotide sequence and share 68% mutual amino acid identity and 30-35% identity with known catecholamine and 5-HT receptors. Saturable binding of 125I-labeled (+)-lysergic acid diethylamide to transiently expressed MR22 in COS-M6 cells was inhibited by ergotamine > methiothepin > 5-carboxamidotryptamine > 5-HT. For REC17, the rank of potency was ergotamine > 5-carboxamidotryptamine > methiothepin > methysergide > 5-HT. Both were insensitive to 5-HT1A, 5-HT1D or 5-HT2 serotonergic ligands [8-hydroxy-2-(di-n-propylamino)tetralin, sumatriptan, and 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane]. The mRNAs encoding MR22 were detected in the CA1 region of hippocampus, the medial habenula, and raphe nuclei. In contrast, mRNAs encoding REC17 were found throughout the rat central nervous system. We propose that REC17 and MR22, designated as 5-HT5 alpha and 5-HT5 beta, represent a distinct subfamily of 5-HT receptors.

Amino Acid Sequence↗
PubMed1994

Selective 5-HT1D alpha serotonin receptor gene expression in trigeminal ganglia: implications for antimigraine drug development.

Pharmacological data suggest that the actions of antimigraine drugs such as sumatriptan may be mediated by 5-HT1D-like serotonin receptors on trigeminovascular nerve endings. We sought molecular evidence for the expression of an mRNA species encoding the 5-HT1D receptor subtype in guinea pig and human trigeminal ganglia, using the polymerase chain reaction with oligonucleotides uniquely homologous to the coding sequences of the 5-HT1B/D family (human 5-HT1D alpha and 5-HT1D beta; rat 5-HT1B). A single band of predicted size was observed in samples from guinea pig trigeminal ganglia; sequence analysis revealed the presence of a single message, which was 85% and 71% identical to the human 5-HT1D alpha and 5-HT1D beta receptor DNA sequences, respectively. Similar analyses of postmortem human trigeminal ganglia revealed the presence of 5-HT1D alpha, but not 5-HT1D beta, receptor message. Inasmuch as one recent report found that mRNA encoding only the 5-HT1D beta receptor subtype was expressed by vascular smooth muscle of the central nervous system, the present findings suggest the importance of developing selective 5-HT1D alpha receptor agonists as a strategy to reduce the risk of myocardial infarction and possibly stroke that complicates the acute treatment of migraine headache.

Animals↗