规格 | 价格 | |
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500mg | ||
1g | ||
Other Sizes |
体外研究 (In Vitro) |
在豚鼠的心房中,单独使用同托品(20 μM)的剂量比为259,与溴化六甲铵配对时,剂量比仅为95.0[1]。胃 (pA2 = 7.13) 和心房 (pA2 = 7.21) 中调节力 (pA2 = 7.07) 和速率 (pA2 = 7.13) 的毒蕈碱受体对同托品具有亲和力[2]。
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体内研究 (In Vivo) |
给大鼠注射含有甲基溴同托品的 9 mm x 5 mm 圆锥形栓剂后,静脉注射乙酰胆碱对血压的影响和迷走神经刺激对脉率的影响被快速阻断[3]。
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动物实验 |
Animal/Disease Models: Male albino rats[3]
Doses: 9 mm x 5 mm conical suppository Route of Administration: By suppository Experimental Results: Blocked cardiovascular responses to vagal stimulation and acetylcholine; 10-20 min after insertion of the suppository the effects of vagal stimulation over a range of 2-16 Hz, 5 V, on pulse rate was virtually abolished and remained unchanged at 45-60 min. |
药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
No pharmacokinetic data available. No pharmacokinetic data available. No pharmacokinetic data available. No pharmacokinetic data available. Metabolism / Metabolites No pharmacokinetic data available. Biological Half-Life No pharmacokinetic data available. |
毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of homatropine hydrobromide during breastfeeding. Anticholinergic drugs might interfere with breastfeeding. A single dose of ophthalmic homatropine hydrobromide is not likely to interfere with breastfeeding; however, during long-term use, observe the infant for signs of decreased lactation (e.g., insatiety, poor weight gain). To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion. Anticholinergic drugs can also reduce serum prolactin in nonnursing women. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. Protein Binding No pharmacokinetic data available. |
参考文献 |
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其他信息 |
Homatropine is a monocarboxylic acid.
Homatropine is an anticholinergic drug that acts as an antagonist at muscarinic acetylcholine receptors. It is present in antitussives, under the trade name Hycodan, in combination with hydrocodone (dihydrocodeinone) bitartrate indicated for the symptomatic relief of cough as oral tablets or solutions. Homatropine is included in subtherapeutic amounts as homatropine methylbromide to discourage deliberate overdosage. Homatropine hydrobromide has been administered as ophthalmic solutions as a cycloplegic to temporarily paralyze accomodation, and to induce mydriasis (the dilation of the pupil); however such therapeutic use has not been approved by the FDA to be safe and effective. Homatropine is a Cholinergic Muscarinic Antagonist. The mechanism of action of homatropine is as a Cholinergic Muscarinic Antagonist. Homatropine is a synthetic tertiary amine alkaloid with antimuscarinic properties. Homatropine, a competitive inhibitor of acetylcholine at the muscarinic receptor, blocks parasympathetic nerve stimulation. See also: Homatropine (annotation moved to). Drug Indication Indicated as an overdose-rescuing agent in combination with hydrocodone antitussive. Indicated for the induction of mydriasis in ophthalmic solutions. FDA Label Mechanism of Action Homatropine is a competitive muscarinic receptor antagonist with a bulky aromatic group in place of the acetyl group of acetylcholine. It is expected to act in similar manner as atropine, producing similar parasympatholytic effects. By blocking muscarinic receptors and cholinergic signalling pathways, homatropine blocks the response of the iris sphincter muscle and cause the pupil to become unresponsive to light upon dilation or mydriasis. It also blocks the accommodative muscle of the ciliary body to cholinergic stimulation. Pharmacodynamics Homatropine is an anticholinergic drug that produces typical anticholinergic effects inducing mydriasis and cycloplegia. Other effects of structurally-related atropine that could also apply to homatropine include inhibition of secretions, tachycardia, relaxation of smooth muscle and central nervous effects including excitation. |
分子式 |
C16H21NO3
|
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分子量 |
275.342844724655
|
精确质量 |
275.152
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CAS号 |
87-00-3
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相关CAS号 |
Homatropine Bromide;51-56-9;Homatropine methylbromide;80-49-9;Homatropine hydrochloride;637-21-8
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PubChem CID |
5282593
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外观&性状 |
Typically exists as solid at room temperature
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密度 |
1.21 g/cm3
|
沸点 |
403.3ºC
|
熔点 |
100ºC
|
闪点 |
197.7ºC
|
LogP |
1.826
|
tPSA |
49.77
|
氢键供体(HBD)数目 |
1
|
氢键受体(HBA)数目 |
4
|
可旋转键数目(RBC) |
4
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重原子数目 |
20
|
分子复杂度/Complexity |
340
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定义原子立体中心数目 |
2
|
SMILES |
O([C@@H]1C[C@@H]2CC[C@@H](N2C)C1)C(=O)C(C1C=CC=CC=1)O
|
InChi Key |
ZTVIKZXZYLEVOL-DGKWVBSXSA-N
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InChi Code |
InChI=1S/C16H21NO3/c1-17-12-7-8-13(17)10-14(9-12)20-16(19)15(18)11-5-3-2-4-6-11/h2-6,12-15,18H,7-10H2,1H3/t12-,13+,14?,15?
|
化学名 |
[(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 2-hydroxy-2-phenylacetate
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
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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溶解度 (体外实验) |
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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溶解度 (体内实验) |
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。
注射用配方
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *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。 View More
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)] 口服配方
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。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 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。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6319 mL | 18.1594 mL | 36.3187 mL | |
5 mM | 0.7264 mL | 3.6319 mL | 7.2637 mL | |
10 mM | 0.3632 mL | 1.8159 mL | 3.6319 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。