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Drotaverine

Drotaverine structure

CAS No:
14009-24-6
Formula:
C24H31NO4
Chemical Name:
Drotaverine
Synonyms:
Isoquinoline,1-[(3,4-diethoxyphenyl)methylene]-6,7-diethoxy-1,2,3,4-tetrahydro-;Isoquinoline,1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydro-;1-[(3,4-Diethoxyphenyl)methylene]-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline;1-(3,4-Diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline;Drotaverine;3′,4′,6,7-Tetraethoxy-1-benzylidene-1,2,3,4-tetrahydroisoquinoline;Drotaverin;3′,4′,6,7-Tetraethoxy-1-benzyliden-1,2,3,4-tetrahydroisoquinoline;Isodihydroperparine;Perparine,isodihydro-;Dihydroisoperparine
Categories:
Active Pharmaceutical Ingredients > Digestive System Drugs

Description

Solid

Drotaverine is a member of isoquinolines.|Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, structurally related to papaverine. Drotaverine is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects. Drotaverine has been shown to possess dose-dependant analgesic effects in animal models. One small study has shown drotaverine to be eliminated mainly non-renally.

Drotaverine Basic Attributes

Molecular Weight：

433.97

Exact Mass：

397.51

EC Number：

1312995-182-4

UNII：

98QS4N58TW

DSSTox ID：

DTXSID60161227

ATC Code：

A - Alimentary tract and metabolism

HScode：

2933499090

Characteristics

PSA：

48.95000

XLogP3：

5.25400

Appearance：

Solid

Density：

1.1507 (rough estimate)

Melting Point：

184 -188ºC

Boiling Point：

520.94°C (rough estimate)

Flash Point：

240.7ºC

Refractive Index：

1.6000 (estimate)

Safety Information

Precautionary statement(s)：

P264, P270, P301+P312, P330, P501

Hazard Statements：

H302

Toxicity

Protein Binding：

80 to 95%

Drug Information

Drug Indication：

Used in the treatment of functional bowel disorders and alleviating pain in renal colic.

Pharmacology：

Drotaverine is a spasmolytic agent by inhibiting PDE4 in smooth muscle cells.

MeSH：

Compounds capable of relieving pain without the loss of CONSCIOUSNESS. (See all compounds classified as Analgesics.)|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.)|Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

Absorption：

Bioavailability is highly variable

Metabolism/Metabolites：

Hepatic

Biological Half-Life：

7 to 12 hours

Mechanism of Action：

Drotaverine inhibits phosphodiesterases hydrolysing cAMP, thereby increasing cAMP concentration, decreasing Ca uptake of the cells and changing the distribution of calcium among the cells. It may also have minor allosteric calcium channel blocking properties.

MeSH Entry Terms：

dihydroisoperparine

Computed Properties

Molecular Weight:397.5
XLogP3:5.4
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:9
Exact Mass:397.22530847
Monoisotopic Mass:397.22530847
Topological Polar Surface Area:49
Heavy Atom Count:29
Complexity:511
Defined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Chlorpheniramine Hydrochloride Taverine CAS 14009-24-6

CAS No.: 14009-24-6

Grade: Pharmaceutical Grade

Content: 99%

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Drotaverine-N-oxide

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