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Home > Encyclopedia > HOMATROPINE METHYL BROMIDE

HOMATROPINE METHYL BROMIDE

pharmaceutical raw materials
HOMATROPINE METHYL BROMIDE structure

HOMATROPINE METHYL BROMIDE 

structure
  • CAS No:

    80-49-9

  • Formula:

    C17H24NO3.Br

  • Chemical Name:

    HOMATROPINE METHYL BROMIDE

  • Synonyms:

    HOMOLONE;HOMATROPINE METHYL BROMIDE;ESOPIN;DL-HOMATROPINE METHYL BROMIDE;ARKITROPIN;8-METHYLHOMATROPINIUM BROMIDE;N-METHYLHOMATROPINIUM BROMIDE;TROPINIUM METHOBROMIDE MANDELATE

  • Categories:

    Active Pharmaceutical Ingredients  >  Nervous System Drugs

Description

Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.target: mAChRIC 50: WKY-E(162.5 nM), SHR-E(170.4nM )In vitro: Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs. Homatropine (20 μM) produces a dose ratio of only 95.0 when combined with hexamethonium in atrium from guinea-pigs.In vivo: : Pre-treatment with homatropine (20 m


Homatropine methylbromide is an organic bromide salt and an azabicycloalkane. It has a role as a muscarinic antagonist, an anti-ulcer drug and an antispasmodic drug.|Homatropine methylbromide is a quaternary ammonium muscarinic acetylcholine receptor antagonist belonging to the group of medicines called anti-muscarinics. Homatropine is used to treat duodenal or stomach ulcers or intestine problems. It can be used together with antacids or other medicine in the treatment of peptic ulcer. It may also be used to prevent nausea, vomiting, and motion sickness.


White or almost white, crystalline powder or colourless crystals


Homatropinemethylbromide, 3 -hydroxy-8-methyl-1 H,5 H-tropaniumbromide mandelate (Novatropine, Mesopin), occurs as a bitter,white, odorless powder and is affected by light. The compoundis readily soluble in water and alcohol but insoluble inether. The pH of a 1% solution is 5.9 and that of a 10% solutionis 4.5. Although a solution of the compound yields a precipitatewith alkaloidal reagents, such as mercuric potassiumiodide test solution, addition of alkali hydroxides or carbonatesdoes not cause the precipitate that occurs with nonquaternarynitrogen salts (e.g., atropine, homatropine).

HOMATROPINE METHYL BROMIDE Basic Attributes

370.28

369.093964

201-284-0

TSCA listed

DTXSID4023127

White to Off-White

29399990

Characteristics

46.53000

3.421

1.21g/cm3

192°C

403.3ºC at 760 mmHg

197.7ºC

1.588

LD50 in mice (mg/kg): 1400 orally, 60 i.p. (Cahen, Tvede)

-20°C Freezer

Safety Information

III

6.1

1544

3

20/21/22

22-26-36

MS9000000

20/21/22

1544

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 65 companies from 4 notifications to the ECHA C&L Inventory.

Drug Information

Used in conjunction with antacids or histamine H2-receptor antagonists in the treatment of peptic ulcers, gastric ulcers and duodenal ulcers, to reduce further gastric acid secretion and delay gastric emptying.

Homatropine methylbromide belongs to the group of medicines called anti-muscarinics. Homatropine is used to treat duodenal or stomach ulcers or intestine problems. It can be used together with antacids or other medicine in the treatment of peptic ulcer. It may also be used to prevent nausea, vomiting, and motion sickness.

Homatropine is a quaternary ammonium muscarinic acetylcholine receptor antagonist. The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Homatropine methylbromide inhibits the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These postganglionic receptor sites are present in the autonomic effector cells of the smooth muscle, cardiac muscle, sinoatrial and atrioventricular nodes, and exocrine glands. Depending on the dose, anticholinergics may reduce the motility and secretory activity of the gastrointestinal system, and the tone of the ureter and urinary bladder and may have a slight relaxant action on the bile ducts and gallbladder.

HOMATROPINE METHYL BROMIDE Use and Manufacturing

Uses

anticholinergic (opthalmic)


Homatropine methylbromide or Methylhomatropine bromide is a quaternary ammonium salt of methylhomatropine. Methylhomatropine is a peripherally acting anticholinergic medication that inhibits muscarinic acetylcholine receptors and thus the parasympathetic nervous system. Methylhomatropine does not cross the blood–brain barrier. Methylhomatropine is used, in addition to papaverine, as component of mild drugs that help "flush" the bile.

8-Azoniabicyclo[3.2.1]octane, 3-[(2-hydroxy-2-phenylacetyl)oxy]-8,8-dimethyl-, bromide (1:1), (3-endo)-: INACTIVE

Computed Properties

Molecular Weight:370.3
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:4
Exact Mass:369.09396
Monoisotopic Mass:369.09396
Topological Polar Surface Area:46.5
Heavy Atom Count:22
Complexity:374
Undefined Atom Stereocenter Count:3
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product is a synthetic anticholinergic drug that blocks acetylcholine, paralyzing the pupillary sphincter and ciliary muscle to cause mydriasis and accommodation paralysis. It is faster and weaker than atropine and is suitable for ophthalmic examination and optometry.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Registered Holders

  • HUBEI BIOCAUSE HEILEN PHARMACEUTICAL CO LTD

    United States United States
    Active
  • C-SQUARED PHARMA LIMITED

    European Union European Union
    Active
  • BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG

    United States United States
    Inactive

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