ISOTHIPENDYL

US Previously Marketed

First approved in 1957

Details

Stereochemistry	RACEMIC
Molecular Formula	C16H19N3S
Molecular Weight	285.407
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(CN1C2=C(SC3=C1N=CC=C3)C=CC=C2)N(C)C

InChI

InChIKey=OQJBSDFFQWMKBQ-UHFFFAOYSA-N

InChI=1S/C16H19N3S/c1-12(18(2)3)11-19-13-7-4-5-8-14(13)20-15-9-6-10-17-16(15)19/h4-10,12H,11H2,1-3H3

HIDE SMILES / InChI

Molecular Formula	C16H19N3S
Molecular Weight	285.407
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://www.drugbank.ca/drugs/DB08802
Curator's Comment: description was created based on several sources, including https://www.drugs.com/international/isothipendyl.html | https://www.ncbi.nlm.nih.gov/pubmed/22677929 | https://www.ncbi.nlm.nih.gov/pubmed/13792589 | https://www.ncbi.nlm.nih.gov/pubmed/14157559

Isothipendyl is a first generation H1 antagonist (antihistamine) and anticholinergic used as an antipruritic. It is nowadays scarcely used in the first line relief of allergies due to the anticholinergic side effect of somnolence but does have some limited use through topical application in the relief of insect bites and related itching (pruritus).

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H1 receptor 315 Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/4150325	Antagonist 2778

Conditions

Condition	Modality	Targets	Highest Phase	Product
Itching 54 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14481215	Primary		Approved 8429	Calmogel Approved Use Unknown

Doses

Dose	Population	Adverse events
1 % single, topical Recommended Dose: 1 % Route: topical Route: single Dose: 1 % Sources: https://pubmed.ncbi.nlm.nih.gov/6138212 Page: p.429	unhealthy, 41 n = 41 Health Status: unhealthy Condition: Dermatisis Age Group: 41 Sex: F Population Size: 41 Sources: https://pubmed.ncbi.nlm.nih.gov/6138212 Page: p.429	Disc. AE: Allergic contact dermatitis... AEs leading to discontinuation/dose reduction: Allergic contact dermatitis Sources: https://pubmed.ncbi.nlm.nih.gov/6138212 Page: p.429
72 mg multiple, oral (max) Studied dose Dose: 72 mg Route: oral Route: multiple Dose: 72 mg Sources: https://pubmed.ncbi.nlm.nih.gov/13792589 Page: p.160	unhealthy n = 72 Health Status: unhealthy Condition: Urticaria \| sensitization dermatitis\|dermatoses Sex: M+F Population Size: 72 Sources: https://pubmed.ncbi.nlm.nih.gov/13792589 Page: p.160	Disc. AE: Weakness generalised... AEs leading to discontinuation/dose reduction: Weakness generalised (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/13792589 Page: p.160

AEs

AE	Significance	Dose	Population
Allergic contact dermatitis	Disc. AE	1 % single, topical Recommended Dose: 1 % Route: topical Route: single Dose: 1 % Sources: https://pubmed.ncbi.nlm.nih.gov/6138212 Page: p.429	unhealthy, 41 n = 41 Health Status: unhealthy Condition: Dermatisis Age Group: 41 Sex: F Population Size: 41 Sources: https://pubmed.ncbi.nlm.nih.gov/6138212 Page: p.429
Weakness generalised	1 patient Disc. AE	72 mg multiple, oral (max) Studied dose Dose: 72 mg Route: oral Route: multiple Dose: 72 mg Sources: https://pubmed.ncbi.nlm.nih.gov/13792589 Page: p.160	unhealthy n = 72 Health Status: unhealthy Condition: Urticaria \| sensitization dermatitis\|dermatoses Sex: M+F Population Size: 72 Sources: https://pubmed.ncbi.nlm.nih.gov/13792589 Page: p.160

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY556280	https://www.001chemical.com/chem/482-15-5
3B Scientific (Wuhan) Corp	3B2-1237	http://www.3bsc.com/index/pro_info.php?id=54953
AHH Chemical co.,ltd	MT-52993	http://www.ahhchemical.com/product/MT-52993.html
Alfa Chemistry	482-15-5	https://www.alfa-chemistry.com/isothipendyl-cas-482-15-5-item-292149.htm
Clearsynth	CS-T-56921	https://www.clearsynth.com/en/CST56921.html
Finetech	FT-0670563	http://www.finetechnology-ind.com/prod/detail/pub/482-15-5.html
Molcore	MC556280	https://www.molcore.com/product/482-15-5
MuseChem	I007385	https://www.musechem.com/product/I007385.html
Smolecule	S530976	http://www.smolecule.com/products/s530976
THE BioTek	bt-270103	https://www.thebiotek.com/product/inhibitors/bt-270103
Yuhao Chemical	RT10332	http://www.chemyuhao.com/482-15-5.html
eNovation Chemicals	D674442	https://www.enovationchem.com/ProductDetails.asp?ProductID=D674442

PubMed

Title	Date	PubMed
Phototoxic and photoprotective effects of topical isothipendyl.	1995 Apr	8546983
Spectrophotometric determination of molybdenum(VI) using isothipendyl hydrochloride and pipazethate hydrochloride in alloy steels and soil samples.	2001 Sep	11708072
Spectrophotometric studies on the investigation of chromium in environmental samples.	2003 Jan	14723280
Bis[N,N-dimethyl-1-(10H-pyrido[3,2-b][1,4]benzothia-zin-10-yl)propan-2-aminium] tetrakis-(thio-cyanato-κN)cobaltate(II).	2010 Jun 16	21587702

Patents

Sample Use Guides

In Vivo Use Guide

The dosage of isothipendyl in children was 6 to 8 mg. daily given as a syrup containing 2 mg. per teaspoonful. In adults the dosage varied from one 4 mg. tablet thrice daily to two 12 mg. sustained-action tablets thrice daily

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Fri Dec 15 18:44:56 GMT 2023` Edited by `admin` on `Fri Dec 15 18:44:56 GMT 2023`
Record UNII	WVZ7K9P0JY
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ISOTHIPENDYL

Official Name

English

D-201

Code

English

UDANTOL

Brand Name

English

ODANTOL

Brand Name

English

(±)-ISOTHIPENDYL

Common Name

English

ISOTHIPENDYL [MI]

Common Name

English

isothipendyl [INN]

Common Name

English

DIMETHYLAMINOISOPROPYLAZAPHENOTHIAZINE

Systematic Name

English

10H-PYRIDO(3,2-B)(1,4)BENZOTHIAZINE-10-ETHANAMINE, N,N,.ALPHA.-TRIMETHYL-

Systematic Name

English

10-(2-DIMETHYLAMINOPROPYL)-10H-PYRIDO(3,2-B)(1,4)BENZOTHIAZINE

Systematic Name

English

10H-PYRIDO(3,2-B)(1,4)BENZOTHIAZINE, 10-(2-(DIMETHYLAMINO)PROPYL)-

Systematic Name

English

ACTAPRONT

Brand Name

English

Isothipendyl [WHO-DD]

Common Name

English

N-DIMETHYLAMINOISOPROPYLTHIOPHENYLPYRIDYLAMINE

Systematic Name

English

AY-56012

Code

English

Classification Tree Code System Code

WHO-ATC

D04AA22