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.

C22H32CL2N6O3S

531.497

458.21

C, 49.72; H, 6.07; Cl, 13.34; N, 15.81; O, 9.03; S, 6.03

170956-82-8

191588-96-2 (HCl);170956-82-8 (2HCl);151140-97-5 (3HCl);151140-96-4; 171171-42-9 (fumarate); 171171-42-9;

O=S(CC1=CC2=C(NC=C2CCCN3CCN(C4=NC=NC=C4OC)CC3)C=C1)(NC)=O.[H]Cl.[H]Cl

LXDKLZKTSZKRLF-UHFFFAOYSA-N

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

1H-Indole-5-methanesulfonamide, 3-(3-(4-(5-methoxy-4-pyrimidinyl)-1-piperazinyl)propyl)-N-methyl-, dihydrochloride

Avitriptan HCl; Avitriptan hydrochloride; Avitriptan dihydrochloride; Avitriptan; BMS 180048; BMS-180048; BMS180048;

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。