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Homatropine methobromide

Homatropine methobromide structure

CAS No:
80-49-9
Formula:
C17H24NO3.Br
Chemical Name:
Homatropine methobromide
Synonyms:
8-Azoniabicyclo[3.2.1]octane,3-[(2-hydroxy-2-phenylacetyl)oxy]-8,8-dimethyl-,bromide (1:1),(3-endo)-;8-Methylhomatropinium bromide;1αH,5αH-Tropanium,3α-hydroxy-8-methyl-,bromide,mandelate;8-Azoniabicyclo[3.2.1]octane,3-[(hydroxyphenylacetyl)oxy]-8,8-dimethyl-,bromide,endo-(±)-;8-Azoniabicyclo[3.2.1]octane,3-[(hydroxyphenylacetyl)oxy]-8,8-dimethyl-,bromide,(3-endo)-;Arkitropin;Camatropine;Esopin;Homapin;Homatromide;Homatropine methylbromide;Malcotran;Mesopin;Methatropin;Methylhomatropine bromide;Novatrin;Novatrine;Novatropine;Sed-Tems;Sethyl;Tropinium methobromide mandelate;Methylhomatropinium bromide;Homatropine methobromide;Methylhomatropine hydrobromide;Helbatropin;Novatropin;Homatrocel;Homatropil;Homolone;Methatropine;8-Azoniabicyclo[3.2.1]octane,3-[(hydroxyphenylacetyl)oxy]-8,8-dimethyl-,bromide,endo-;NSC 34399;42522-67-8;55198-66-8;58725-74-9;1786394-41-9
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.

Homatropine methobromide Basic Attributes

Molecular Weight：

370.28

Exact Mass：

369.093964

EC Number：

201-284-0

DSSTox ID：

DTXSID4023127

HScode：

29399990

Characteristics

PSA：

46.53000

XLogP3：

3.421

Density：

1.21g/cm3

Melting Point：

191-192 °C (decomp)

Boiling Point：

403.3ºC at 760 mmHg

Flash Point：

197.7ºC

Refractive Index：

1.588

Toxicity：

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

Safety Information

Hazard category：

6.1

Transport codes：

1544

wgk germany：

hazard class code：

20/21/22

safety instructions：

22-26-36

RTECS Number：

MS9000000

GHS Classification：

|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

Drug Indication：

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.

Pharmacology：

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.

Mechanism of Action：

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 methobromide Use and Manufacturing

Uses

anticholinergic (opthalmic)

Manufacturing Info：

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

Homatropine Hydrobromide
Ingredients	Homatropine Methyl Bromide
Manufacturer	China Resources Double-Crane Pharmaceutical Co., Ltd.

Homatropine Hydrobromide
Ingredients	Homatropine Methyl Bromide
Manufacturer	Chengdu Shidai No.1 Pharmaceutical Co., Ltd.

Registered Holders

HUBEI BIOCAUSE HEILEN PHARMACEUTICAL CO LTD

United States
Active
C-SQUARED PHARMA LIMITED

European Union
Active
BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG

United States
Inactive

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