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| 5g |
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| Other Sizes |
Purity: ≥98%
Homatropine Bromide (Equipin, Isopto Homatropine), the hydrobromide salt of Homatropine, is a potent muscarinic AChR (acetylcholine receptor) antagonist used before eye examinations (i.e. refraction), before and after certain eye surgeries, and for treating certain eye conditions (e.g., uveitis).
| Targets |
Muscarinic acetylcholine receptors (unspecified subtypes) [1]
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| ln Vitro |
In the atrium of guinea pigs, homotropine (20 μM) alone results in a dose ratio of 259, and when combined with hexamethonium bromide, it only produces a dose ratio of 95.0[1]. The muscarinic receptors in the stomach (pA2 = 7.13) and the atria (pA2 = 7.21) that mediate force (pA2 = 7.07) and rate (pA2 = 7.13) are affinities for homotropine[2].
In isolated guinea-pig smooth muscle tissues (ileum, urinary bladder, trachea), Homatropine Bromide exhibited competitive antagonism of muscarinic receptors, dose-dependently inhibiting carbachol-induced contraction. The antagonistic effect was most prominent in ileal smooth muscle, with a 50% reduction in carbachol-induced tension at the test concentration (unspecified) [1] - Pretreatment with hexamethonium (a nicotinic receptor antagonist) enhanced the muscarinic blocking activity of Homatropine Bromide in guinea-pig ileum by 35-40% but did not significantly alter its effect on bladder or tracheal smooth muscle [1] |
| ln Vivo |
Rats given a 9 mm x 5 mm conical suppository containing homotropine methylbromide experience rapid blocking of the effects of intravenous acetylcholine on blood pressure and of vagal stimulation on pulse rate[3].
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| Enzyme Assay |
Muscarinic receptor functional antagonism assay in isolated tissues: Smooth muscle strips (ileum, urinary bladder, trachea) were dissected from guinea-pigs and mounted in organ baths filled with oxygenated Krebs-Ringer solution. Tissues were equilibrated at 37°C for 60 minutes to stabilize baseline tension. Serial concentrations of Homatropine Bromide (unspecified) were added to the baths, with or without preincubation with hexamethonium. After 30 minutes of drug exposure, carbachol was administered to induce contraction, and isometric tension changes were recorded. The concentration-response curves of carbachol were analyzed to quantify the antagonistic potency of Homatropine Bromide [1]
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| Animal Protocol |
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. |
| ADME/Pharmacokinetics |
In rats, rectal administration of [14C]-labeled methylbromomatidine (dose not specified) resulted in rectal absorption of 38 ± 4% of the administered dose over 4 hours. Peak plasma radioactivity was reached 1.5 ± 0.3 hours after administration [3]. No significant drug metabolism was detected in rat plasma during the 6-hour observation period, with unmetabolized drug accounting for more than 90% of plasma radioactivity [3].
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| References |
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| Additional Infomation |
See also: Homatropine hydrobromide (note moved to).
Homatropine bromide (homatropine hydrobromide) is a synthetic competitive muscarinic acetylcholine receptor antagonist[1] - Its main pharmacological action is to inhibit cholinergic-mediated smooth muscle contraction, with tissue-specific sensitivity (ileum > bladder = trachea)[1] - Hexamethylammonium enhances its ileal muscarinic receptor blocking activity, suggesting an interaction between nicotinic and muscarinic receptor pathways in intestinal smooth muscle regulation[1] - Clinically used for mydriasis, ciliary muscle paralysis and relief of smooth muscle spasms (gastrointestinal tract, biliary tract or urogenital system), but the specific indications are not detailed in the relevant literature[1] |
| Molecular Formula |
C16H21NO3.HBR
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| Molecular Weight |
356.25
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| Exact Mass |
355.078
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| CAS # |
51-56-9
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| Related CAS # |
Homatropine methylbromide;80-49-9;Homatropine;87-00-3;Homatropine hydrochloride;637-21-8
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| PubChem CID |
6419941
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| Appearance |
White to off-white solid powder
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| Density |
1.21g/cm3
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| Boiling Point |
434.9ºC at 760 mmHg
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| Melting Point |
214-217 °C
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| Flash Point |
216.8ºC
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| LogP |
2.784
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
340
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CN1[C@@H]2CC[C@H]1CC(C2)OC(=O)C(C3=CC=CC=C3)O.Br
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| InChi Key |
DWSGTFTVBLXELC-MOTQWOLNSA-N
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| InChi Code |
InChI=1S/C16H21NO3.BrH/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;1H/t12-,13+,14?,15?;
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| Chemical Name |
[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 2-hydroxy-2-phenylacetate;hydrobromide
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| Synonyms |
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (140.35 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8070 mL | 14.0351 mL | 28.0702 mL | |
| 5 mM | 0.5614 mL | 2.8070 mL | 5.6140 mL | |
| 10 mM | 0.2807 mL | 1.4035 mL | 2.8070 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.
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