ZINDOTRINE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C11H15N5
Molecular Weight	217.2703
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CC(=NN2C=NN=C12)N3CCCCC3

InChI

InChIKey=YYHWOTFWBVRTQD-UHFFFAOYSA-N

InChI=1S/C11H15N5/c1-9-7-10(15-5-3-2-4-6-15)14-16-8-12-13-11(9)16/h7-8H,2-6H2,1H3

HIDE SMILES / InChI

Molecular Formula	C11H15N5
Molecular Weight	217.2703
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3307547 | https://adisinsight.springer.com/drugs/800000052 | https://www.ncbi.nlm.nih.gov/pubmed/3229340

Zindotrine [MDL 257] is a phosphodiesterase inhibitor that was undergoing phase II clinical trials, with Aventis Pharma, as an antiasthmatic. However, no recent study has been reported. Hoechst Marion Roussel originally developed the drug. Efficacy and cardiovascular effects of a single 300 mg oral dose of zindotrine were compared with placebo in a two-period, double-blind, and crossover trial. A single dose of zindotrine 300 mg provided effective bronchodilator action with a relatively prolonged response and tolerable side effects

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Phosphodiesterase 1 Target ID: Phosphodiesterase Sources: https://adisinsight.springer.com/drugs/800000052	Inhibitor 8297

PubMed

Title	Date	PubMed
The effect of oral zindotrine (MDL-257), a bronchial smooth muscle relaxant, on histamine airways responsiveness in asymptomatic asthmatics.	1987 Sep	3307547
Single-dose efficacy and safety of zindotrine, a new oral bronchodilator.	1988 Oct	3229340

Patents

Sample Use Guides

In Vivo Use Guide

Histamine inhalation challenges were performed before (control) and 45, 150, and 300 minutes after zindotrine (200 and 300 mg), or the corresponding dose of placebo was administered orally in a randomized, double-blind crossover fashion. When compared to the control state, the 300-mg zindotrine dose markedly lowered histamine airway responsiveness. Orally administered zindotrine lowers airways responsiveness to inhaled histamine in asymptomatic asthmatics in a dose-dependent and time-dependent fashion.

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:05:03 GMT 2023` Edited by `admin` on `Fri Dec 15 15:05:03 GMT 2023`
Record UNII	VQM3328PO0
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ZINDOTRINE

Official Name

English

zindotrine [INN]

Common Name

English

MDL 257

Code

English

MDL-257

Code

English

1,2,4-TRIAZOLO(4,3-B)PYRIDAZINE, 8-METHYL-6-(1-PIPERIDINYL)-

Systematic Name

English

ZINDOTRINE [USAN]

Common Name

English

8-METHYL-6-(1-PIPERIDINYL)-S-TRIAZOLO(4,3-B)PYRIDAZINE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C319