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Alverine citrate

Alverine citrate structure

CAS No:
5560-59-8
Formula:
C20H27N.C6H8O7
Chemical Name:
Alverine citrate
Synonyms:
Benzenepropanamine,N-ethyl-N-(3-phenylpropyl)-,2-hydroxy-1,2,3-propanetricarboxylate (1:1);Dipropylamine,N-ethyl-3,3′-diphenyl-,citrate (1:1);Alverine citrate;Gamatran citrate;Spacolin;Antispasmin;Prophelan;Gamatran;Proverine;Spasmonal;Spasmaverine;Profenine;Calmabel;NSC 35459;144-30-9
Categories:
Organic Chemistry > Amides

Description

Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.

Alverine citrate is the citrate salt of alverine, resulting from the reaction of equimolar amounts of alvarine and citric acid. An antispasmodic that acts directly on intestinal and uterine smooth muscle, it is used in the treatment of irritable bowel syndrome. It has a role as a cholinergic antagonist and an antispasmodic drug. It is a citrate salt and an organoammonium salt. It contains an alverine(1+).

Alverine citrate Basic Attributes

Molecular Weight：

473.56

Exact Mass：

473.24100

EC Number：

226-929-3

UNII：

9JFB58YK1E

NSC Number：

755859|35459

DSSTox ID：

DTXSID3045562

HScode：

2921499090

Characteristics

PSA：

135

XLogP3：

3.32540

Appearance：

COA

Melting Point：

100-102°

Boiling Point：

358.8°C at 760 mmHg

Flash Point：

174.4ºC

Collision Cross Section：

168.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

safety instructions：

24/25

Precautionary statement(s)：

P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P312, P322, P330, P363, P501

Hazard Statements：

H302

GHS Classification：

|Danger|H301 (25%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P310, P301+P312, P302+P352, P304+P312, P304+P340, P312, P321, P322, P330, P363, P405, and P501|Aggregated GHS information provided by 5 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

MeSH：

Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS. (See all compounds classified as Parasympatholytics.)

MeSH Entry Terms：

alverine

Alverine citrate Use and Manufacturing

Methods of Manufacturing

At temperatures between 45 and 50 ° C, The citric acid (57.5g, 0.3mol)In 240 mL of ethyl acetateAnd 120 mL of isopropyl alcoholOf the mixed solvent, The above obtained alvain free base (85 g, 0.3 mol)In 100 mL of ethyl acetate, Drop finished, Continue to reflux state stirring 0.5 ~ 1h, Natural cooling to 20 ~ 30 ° C, A large amount of white solid precipitated, Filter, washing, Get citrate alverine about128g. The above-obtained aliskine citrate was about 128 g, and the mixture was stirred at a temperature of 45 to 50 ° C and dissolved in a mixed solvent of N-methylpyrrolidone (260 mL) and water (260 mL). The appropriate amount of DMF was about 55 mL, 0 ° C, static crystallization of 4-5h, filter precipitation of crystals, filtration precipitation of crystals, 35 ~ 40 ° C vacuum drying, humidity control in the 20 ~ 40percent relative humidity, that was white solid 122g, the yield of about 92percent, HPLC purity 99.7percent.13.5 g of the above liquid was dissolved in 100 ml of absolute ethanol and dissolved by stirring. Then, 9.2 g (0.048 mol) of citric acid was dissolved in 100 ml of absolute ethanol, and the solid was stirred at room temperature to precipitate a solid.Filtering, washing and drying.Recrystallization from ethanol to obtain 15.2g of Alvulin citrate.Yield: 66.9percent.

Uses

anticholinergic

Computed Properties

Molecular Weight:473.6
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:14
Exact Mass:473.24135246
Monoisotopic Mass:473.24135246
Topological Polar Surface Area:135
Heavy Atom Count:34
Complexity:442
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Smona is a synthetic derivative of papaverine, which acts directly on smooth muscle. It is a selective smooth muscle relaxant. Its mechanism of action is to affect the potential sensitivity of ion channels and the metabolic pathway of phosphate and inositol. This product selectively acts on the smooth muscles of the gastrointestinal tract, uterus, and reproductive and urinary tract organs, and has almost no effect on the tracheal and vascular smooth muscles at normal doses. The antispasmodic effect on smooth muscle is about 2.5 to 3 times that of papaverine. The inhibition of histamine reaction is 5 times that of atropine, but the inhibition of acetylcholine reaction is only one ten-thousandth of atropine. Therefore, there is no contraindication for patients with glaucoma and prostatic hypertrophy. This product is not addictive.

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

Alverine Citrate Capsules
Ingredients	The main ingredient of this product is Alverine Citrate Chemical Name: N-Ethyl-3,3'-Diphenyldipropylamine Citrate Molecular Formula: C20H27N.C6H8O7
Specifications	60 mg

Alverine Citrate Capsules
Ingredients	Alverine citrate.
Indication	Drug interactions may occur if used with other drugs. Please consult your doctor or pharmacist for details.
Specifications	60 mg

Granisetron Hydrochloride and Sodium Chloride Injection
Ingredients	The chemical composition is alverine citrate. The chemical name is N-ethyl-3,3'-diphenyldipropylamine citrate. The molecular formula is C20H27N.C6H8O7. The molecular weight is 473.57.
Indication	Tricyclic antidepressants and similar drugs, procainamide or its derivatives, H1 antihistamines can enhance the effect of this drug. Systemic cholinergic drugs can reduce the effect of this drug.
Specifications	100 ml: Granisetron hydrochloride [C18H24N4O] 3 mg and sodium chloride 0.9 g
Manufacturer	Fuzhou FU Yao Pharmaceutical Co., Ltd.

Registered Holders

PROCOS S.P.A.

Italy
Inactive

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