Almotriptan Malate
Axert · Almogran · PNU 180638 · PNU-180638 · Almotriptan · LAS-31416 Malate · 1-[[[3-[2-(dimeth · Amotriptan malate
식별자 및 물리적 특성
| CAS No. | 181183-52-8 |
|---|---|
| 분자식 | C21H31N3O7S |
| 평균 분자량 | 469.56 g/mol |
| 단동위원소 질량 | 469.18827133 g/mol |
| SMILES | CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N3CCCC3)cc12.O=C(O)CC(O)C(=O)O |
| InChIKey | QHATUKWEVNMHRY-UHFFFAOYSA-N |
| PubChem CID | 123607 |
| ChEMBL | CHEMBL1200521 |
| ChEBI | CHEBI:53781 |
| EC No. | 815-382-1 |
| DTXSID | DTXSID1044225 |
화학 및 물리적 성질
| 녹는점 | 170-172°C |
|---|---|
| 저장 조건 | 2-8°C |
| 용해도 | 염기성 알코올(약간 용해됨), DMSO(약간 용해됨), 메탄올(약간 용해됨, 가열) |
| 물리적 상태 | 가루 |
| 색상 | 흰색에서 베이지색 |
| 용해도 | H2O: 10mg/mL, clear |
| InChIKey | QHATUKWEVNMHRY-UHFFFAOYSA-N |
| SMILES | [S](=O)(=O)(N3CCCC3)Cc1cc2c([nH]cc2CCN(C)C)cc1.OC(CC(=O)O)C(=O)O |
화학적 성질
Pale Yellow Solid
안전 및 규제
| 수질 위해 등급(WGK) | WGK 3 |
|---|---|
| 관세 코드 | 2935904000 |
| 저장 분류 | 11 - Combustible Solids |
용도
개요
Almotriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (IC50s = 12 and 13 nM, respectively, in a radioligand binding assay). It is selective for human 5-HT1B and 5-HT1D receptors over rat 5-HT1A and human 5-HT2A and 5-HT4 receptors (IC50s = 0.85, 25.1, and 140 μM, respectively). Almotriptan induces contractions in isolated canine saphenous veins (EC50 = 394 nM) but not isolated rabbit renal or mesenteric arteries. It increases carotid vascular resistance in anesthetized cats (ED100 = 11 μg/kg, i.v.) without increasing blood pressure or heart rate. Formulations containing almotriptan have been used in the treatment of migraine headaches.
용도
Almotriptan is a serotonin 5HT1B /1D-receptor agonist used for treatment of migraine.
일반 설명
Almotriptan, marketed in 2000, has the highest oralbioavailability among all triptans. It is metabolizedby both MAO-A and CYP3A4, thus has a more favorableside effects profile when compared with sumatriptan.However, it is only available in a 12.5 mg tablet form.