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References |
1: Vyhlídalová B, Krasulová K, Pečinková P, Poulíková K, Vrzal R, Andrysík Z, Chandran A, Mani S, Dvorak Z. Antimigraine Drug Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor That Induces CYP1A1 in Hepatic and Intestinal Cells. Int J Mol Sci. 2020 Apr 17;21(8):2799. doi: 10.3390/ijms21082799. PMID: 32316498; PMCID: PMC7216230. 2: Fang W, Bauer F, Dong Y, Breit B. A domino reaction for generating β-aryl aldehydes from alkynes by substrate recognition catalysis. Nat Commun. 2019 Oct 25;10(1):4868. doi: 10.1038/s41467-019-12770-w. PMID: 31653836; PMCID: PMC6814718. 3: Puente J, Jaque M, Carrasco C, Cruz C, Valenzuela M, Wolf M, Mosnaim A. Triptan drugs, natural killer cell cytotoxicity, and neutrophils pro-matrix metalloproteinase-9 secretion. Headache. 2008 Nov-Dec;48(10):1482-9. doi: 10.1111/j.1526-4610.2008.01136.x. Epub 2008 May 9. PMID: 18479418. 4: Schmidt LE, Dalhoff K. Food-drug interactions. Drugs. 2002;62(10):1481-502. doi: 10.2165/00003495-200262100-00005. PMID: 12093316. 5: Bhalla P, Sharma HS, Wurch T, Pauwels PJ, Saxena PR. Molecular cloning and expression of the porcine trigeminal ganglion cDNA encoding a 5-ht(1F) receptor. Eur J Pharmacol. 2002 Feb 1;436(1-2):23-33. doi: 10.1016/s0014-2999(01)01605-3. PMID: 11834243. 6: Maslov LN, Krylatov AV, Lishmanov AIu, Solenkova NV, Bogomaz SA. Tolerantnost' serdtsa krys k aritmogennym vozdeĭstviiam v usloviiakh farmakologicheskoĭ aktivatsii K(ATP)-kanalov [Myocardial tolerance to arrhythmogenic exposure and pharmacological activation of K(ATP)-channels in rats]. Eksp Klin Farmakol. 2001 Mar-Apr;64(2):41-4. Russian. PMID: 11548447. 7: Knight YE, Edvinsson L, Goadsby PJ. Blockade of calcitonin gene-related peptide release after superior sagittal sinus stimulation in cat: a comparison of avitriptan and CP122,288. Neuropeptides. 1999 Feb;33(1):41-6. doi: 10.1054/npep.1999.0009. PMID: 10657470. 8: Roon KI, Maassen Van Den Brink A, Ferrari MD, Saxena PR. Bovine isolated middle cerebral artery contractions to antimigraine drugs. Naunyn Schmiedebergs Arch Pharmacol. 1999 Nov;360(5):591-6. doi: 10.1007/s002109900095. PMID: 10598799. 9: Nilsson T, Longmore J, Shaw D, Olesen IJ, Edvinsson L. Contractile 5-HT1B receptors in human cerebral arteries: pharmacological characterization and localization with immunocytochemistry. Br J Pharmacol. 1999 Nov;128(6):1133-40. doi: 10.1038/sj.bjp.0702773. PMID: 10578124; PMCID: PMC1571736. 10: Sharma A, Jusko WJ, Fulmor IE, Norton J, Uderman HD, Salazar DE. Pharmacokinetics and pharmacodynamics of avitriptan during intravenous administration in healthy subjects. J Clin Pharmacol. 1999 Jul;39(7):685-94. doi: 10.1177/00912709922008326. PMID: 10392323. 11: Jhee SS, Salazar DE, Ford NF, Fulmor IE, Sramek JJ, Cutler NR. A double- blind, randomized, crossover assessment of blood pressure following administration of avitriptan, sumatriptan, or placebo to patients with mild to moderate hypertension. Cephalalgia. 1999 Mar;19(2):95-9. doi: 10.1046/j.1468-2982.1999.019002095.x. PMID: 10214534. 12: Swan L, Hood S, Birnie DH, Muir DF, McCann GP, Hillis WS. The haemodynamic effect of the 5HT1 agonist BMS-180048: a class effect of triptans? Br J Clin Pharmacol. 1999 Feb;47(2):189-94. doi: 10.1046/j.1365-2125.1999.00875.x. PMID: 10190654; PMCID: PMC2014163. 13: Dahlöf CG, Falk L, Risenfors M, Lewis CP. 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. Cephalalgia. 1998 Oct;18(8):546-51. doi: 10.1046/j.1468-2982.1998.1808546.x. PMID: 9827246. 14: Marathe PH, Sandefer EP, Kollia GE, Greene DS, Barbhaiya RH, Lipper RA, Page RC, Doll WJ, Ryo UY, Digenis GA. In vivo evaluation of the absorption and gastrointestinal transit of avitriptan in fed and fasted subjects using gamma scintigraphy. J Pharmacokinet Biopharm. 1998 Feb;26(1):1-20. doi: 10.1023/a:1023236823320. PMID: 9773390. 15: Marathe PH, Greene DS, Kollia GD, Barbhaiya RH. Evaluation of the effect of food on the pharmacokinetics of avitriptan. Biopharm Drug Dispos. 1998 Sep;19(6):381-94. doi: 10.1002/(sici)1099-081x(199809)19:6<381::aid- bdd118>3.0.co;2-j. PMID: 9737819. 16: MaassenVanDenBrink A, Reekers M, Bax WA, Ferrari MD, Saxena PR. Coronary side-effect potential of current and prospective antimigraine drugs. Circulation. 1998 Jul 7;98(1):25-30. doi: 10.1161/01.cir.98.1.25. PMID: 9665056. 17: Cutler NR, Salazar DE, Jhee SS, Fulmor IE, Ford N, Smith RA, Sramek JJ. Pharmacokinetics and pharmacodynamics of avitriptan in patients with migraine after oral dosing. Headache. 1998 Jun;38(6):446-52. doi: 10.1046/j.1526-4610.1998.3806446.x. PMID: 9664749. 18: Marathe PH, Greene DS, Lee JS, Barbhaiya RH. Assessment of effect of food, gender, and intra-subject variability in the pharmacokinetics of avitriptan. Biopharm Drug Dispos. 1998 Apr;19(3):153-7. doi: 10.1002/(sici)1099-081x(199804)19:3<153::aid-bdd90>3.0.co;2-t. PMID: 9569997. 19: Marathe PH, Greene DS, Kollia GD, Barbhaiya RH. A pharmacokinetic interaction study of avitriptan and propranolol. Clin Pharmacol Ther. 1998 Mar;63(3):367-78. doi: 10.1016/S0009-9236(98)90168-0. PMID: 9542480. 20: Marathe PH, Greene DS, Kollia GD, Barbhaiya RH. The effects of age and gender on the single dose pharmacokinetics of avitriptan administered to healthy volunteers. J Clin Pharmacol. 1997 Oct;37(10):937-45. doi: 10.1002/j.1552-4604.1997.tb04268.x. PMID: 9505985.
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Molecular Formula |
C22H32CL2N6O3S
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Molecular Weight |
531.497
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Exact Mass |
458.21
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Elemental Analysis |
C, 49.72; H, 6.07; Cl, 13.34; N, 15.81; O, 9.03; S, 6.03
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CAS # |
170956-82-8
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Related CAS # |
191588-96-2 (HCl);170956-82-8 (2HCl);151140-97-5 (3HCl);151140-96-4; 171171-42-9 (fumarate); 171171-42-9;
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Appearance |
Solid powder
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SMILES |
O=S(CC1=CC2=C(NC=C2CCCN3CCN(C4=NC=NC=C4OC)CC3)C=C1)(NC)=O.[H]Cl.[H]Cl
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InChi Key |
LXDKLZKTSZKRLF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H30N6O3S.2ClH/c1-23-32(29,30)15-17-5-6-20-19(12-17)18(13-25-20)4-3-7-27-8-10-28(11-9-27)22-21(31-2)14-24-16-26-22;;/h5-6,12-14,16,23,25H,3-4,7-11,15H2,1-2H3;2*1H
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Chemical Name |
1H-Indole-5-methanesulfonamide, 3-(3-(4-(5-methoxy-4-pyrimidinyl)-1-piperazinyl)propyl)-N-methyl-, dihydrochloride
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Synonyms |
Avitriptan HCl; Avitriptan hydrochloride; Avitriptan dihydrochloride; Avitriptan; BMS 180048; BMS-180048; BMS180048;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8815 mL | 9.4073 mL | 18.8147 mL | |
5 mM | 0.3763 mL | 1.8815 mL | 3.7629 mL | |
10 mM | 0.1881 mL | 0.9407 mL | 1.8815 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.