avitriptan: an anti-migraine agent; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 133081 |
| CHEMBL ID | 2110755 |
| CHEBI ID | 177844 |
| SCHEMBL ID | 147315 |
| MeSH ID | M0269988 |
| Synonym |
|---|
| CHEBI:177844 |
| 1-[3-[3-[4-(5-methoxypyrimidin-4-yl)piperazin-1-yl]propyl]-1h-indol-5-yl]-n-methylmethanesulonamide |
| 151140-96-4 |
| avitriptan [inn] |
| 3-(3-(4-(5-methoxy-4-pyrimidinyl)-1-piperazinyl)propyl)-n-methylindole-5-methanesulfonamide |
| avitriptan |
| 1h-indole-5-methanesulfonamide, 3-(3-(4-(5-methoxy-4-pyrimidinyl)-1-piperazinyl)propyl)-n-methyl- |
| L012862 |
| 1-[3-[3-[4-(5-methoxypyrimidin-4-yl)piperazin-1-yl]propyl]-1h-indol-5-yl]-n-methylmethanesulfonamide |
| 6rs056l04p , |
| unii-6rs056l04p |
| SCHEMBL147315 |
| WRZVGHXUPBWIOO-UHFFFAOYSA-N |
| 4-(5-methoxy-4-pyrimidinyl)-1-[3-[5-[[(methylamino)sulfonyl]methyl]-1h-indol-3-yl]propyl]piperazine |
| CHEMBL2110755 |
| DTXSID60164718 |
| Q4829012 |
| bms-180,048 |
| gtpl10446 |
| bms180048 |
| 151140-96-4 (free base) |
| 1h-indole-5-methanesulfonamide, 3-[3-[4-(5-methoxy-4-pyrimidinyl)-1-piperazinyl]propyl]-n-methyl- |
Avitriptan (BMS-180048) is a 5-HT1-like receptor agonist for the treatment of migraine.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Avitriptan is a new 5-HT1-like agonist with abortive antimigraine properties. " | ( Disposition of [14C]avitriptan in rats and humans. Barbhaiya, RH; Greene, DS; Marathe, PH, 1997) | 2.06 |
| "Avitriptan (BMS-180048) is a 5-HT1-like receptor agonist for the treatment of migraine. " | ( Pharmacokinetics and pharmacodynamics of avitriptan in patients with migraine after oral dosing. Cutler, NR; Ford, N; Fulmor, IE; Jhee, SS; Salazar, DE; Smith, RA; Sramek, JJ, 1998) | 2.01 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Forty-five patients (88%) reported at least one adverse event and 23 (45%) experienced pressure, tightness, and/or pain in the chest, neck, and/or throat after administration of avitriptan." | ( Safety trial with the 5HT1B/1D agonist avitriptan (BMS-180048) in patients with migraine who have experienced pressure, tightness, and/or pain in the chest, neck, and/or throat following sumatriptan. Dahlöf, CG; Falk, L; Lewis, CP; Risenfors, M, 1998) | 0.76 |
The study was conducted to assess the bioavailability of avitriptan after a standard high fat meal, in relation to gastrointestinal transit.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Absolute bioavailability was 19." | ( Disposition of [14C]avitriptan in rats and humans. Barbhaiya, RH; Greene, DS; Marathe, PH, 1997) | 0.62 |
| " A series of studies were conducted in humans to assess the effect of timing of meal, type of meal, gastric pH, change in the formulation and dose on the bioavailability of avitriptan." | ( Evaluation of the effect of food on the pharmacokinetics of avitriptan. Barbhaiya, RH; Greene, DS; Kollia, GD; Marathe, PH, 1998) | 0.74 |
| "The study was conducted to assess the bioavailability of avitriptan after a standard high fat meal, in relation to gastrointestinal transit." | ( In vivo evaluation of the absorption and gastrointestinal transit of avitriptan in fed and fasted subjects using gamma scintigraphy. Barbhaiya, RH; Digenis, GA; Doll, WJ; Greene, DS; Kollia, GE; Lipper, RA; Marathe, PH; Page, RC; Ryo, UY; Sandefer, EP, 1998) | 0.78 |
Avitriptan was administered as a 50 mg 14C-labeled solution after a standard high fat meal. Peak plasma concentrations were achieved 1 to 2 hours following dosing in migraine and pain-free states for all doses.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Serial blood samples were collected over 24 h after dosing and analyzed by a validated HPLC method for avitriptan." | ( Assessment of effect of food, gender, and intra-subject variability in the pharmacokinetics of avitriptan. Barbhaiya, RH; Greene, DS; Lee, JS; Marathe, PH, 1998) | 0.73 |
| " Peak plasma concentrations of avitriptan were achieved 1 to 2 hours following dosing in migraine and pain-free states for all doses." | ( Pharmacokinetics and pharmacodynamics of avitriptan in patients with migraine after oral dosing. Cutler, NR; Ford, N; Fulmor, IE; Jhee, SS; Salazar, DE; Smith, RA; Sramek, JJ, 1998) | 0.85 |
| " When administered as a 50 mg 14C-labeled solution after a standard high fat meal, bioavailability of avitriptan decreased although the decrease was less compared with that observed for a capsule dosage form." | ( Evaluation of the effect of food on the pharmacokinetics of avitriptan. Barbhaiya, RH; Greene, DS; Kollia, GD; Marathe, PH, 1998) | 0.76 |
| Class | Description |
|---|---|
| tryptamines | Tryptamine and its substitution derivatives. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 17 (94.44) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 1 (5.56) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (20.12) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 13 (68.42%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (31.58%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||