BENPROPERINE PHOSPHATE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C21H27NO.H3O4P
Molecular Weight	407.4404
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

OP(O)(O)=O.CC(COC1=C(CC2=CC=CC=C2)C=CC=C1)N3CCCCC3

InChI

InChIKey=MCVUURBOSHQXMK-UHFFFAOYSA-N

InChI=1S/C21H27NO.H3O4P/c1-18(22-14-8-3-9-15-22)17-23-21-13-7-6-12-20(21)16-19-10-4-2-5-11-19;1-5(2,3)4/h2,4-7,10-13,18H,3,8-9,14-17H2,1H3;(H3,1,2,3,4)

HIDE SMILES / InChI

Description

Benproperine (Cofrel) is a cough suppressant. It is used for symptomatic relief of cough. Cofrel is 2-4 times as potent as codeine in suppressing cough in animals. It acts peripherally by blocking afferent sensory nerve impulses originating from receptors in the lungs and pleura.

Originator

Approval Year

Conditions

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cough 106	Palliative		Approved 8,583	Cofrel

C_max

Value	Dose	Analyte	Population
333 ng/mL	60 mg single, oral	BENPROPERINE, (S)- plasma	Homo sapiens
153 ng/mL	60 mg single, oral	BENPROPERINE, (R)- plasma	Homo sapiens
146.4 ng/mL	80 mg single, oral	BENPROPERINE plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
4257 ng × h/mL	60 mg single, oral	BENPROPERINE, (S)- plasma	Homo sapiens
2010 ng × h/mL	60 mg single, oral	BENPROPERINE, (R)- plasma	Homo sapiens
5234.31 ng × h/mL	80 mg single, oral	BENPROPERINE plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
17 h	60 mg single, oral	BENPROPERINE, (S)- plasma	Homo sapiens
14 h	60 mg single, oral	BENPROPERINE, (R)- plasma	Homo sapiens
24.7 h	80 mg single, oral	BENPROPERINE plasma	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
80 mg single, oral Highest studied dose	healthy, ADULT

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PubMed

Title	Date	PubMed
No data available in table

Patents

Sample Use Guides

In Vivo Use Guide

1 or 2 tablets 3 times daily, according to severity of cough. Tablets should be swallowed whole and not chewed.

Route of Administration: Oral

In Vitro Use Guide

10(-5) g/ml of Benproperine (ASA 158/5) caused remarkable reduction of the contraction of the tracheal muscle preparation of a guinea pig caused by histamine HCl.

Show entries

Name

Type

Language

BENPROPERINE TRIHYDROGEN PHOSPHATE

Preferred Name

English

BENPROPERINE PHOSPHATE

Common Name

English

ASA-158/5

Code

English

ASA 158/5

Code

English

BENPROPERINE PHOSPHATE [JAN]

Common Name

English

Showing 1 to 5 of 9 entries

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Show entries

Code System

Code

Type

Description

MERCK INDEX

m2321

PRIMARY

Merck Index

CAS

3563-76-6

SUPERSEDED

ECHA (EC/EINECS)

222-635-4

ALTERNATIVE

EVMPD

SUB00705MIG

PRIMARY

ChEMBL

CHEMBL2105910

PRIMARY

Showing 1 to 5 of 12 entries

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ACTIVE MOIETY


					3AA6IZ48YK

BENPROPERINE

SUBSTANCE RECORD


					S831Z48C5W

BENPROPERINE PHOSPHATE

SMILES

InChI

Originator

Approval Year

Conditions

Cmax

AUC

T1/2

Doses

PubMed

Patents

Sample Use Guides

C_max

T_1/2