RTI-336 FREE BASE

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H25ClN2O
Molecular Weight	392.921
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1[C@H]2CC[C@@H]1[C@H]([C@H](C2)C3=CC=C(Cl)C=C3)C4=CC(=NO4)C5=CC=C(C)C=C5

InChI

InChIKey=AUXUFNHAVGIVDC-IKJKNFHUSA-N

InChI=1S/C24H25ClN2O/c1-15-3-5-17(6-4-15)21-14-23(28-26-21)24-20(16-7-9-18(25)10-8-16)13-19-11-12-22(24)27(19)2/h3-10,14,19-20,22,24H,11-13H2,1-2H3/t19-,20+,22+,24-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C24H25ClN2O
Molecular Weight	392.921
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	4 / 4
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30042675 | https://www.ncbi.nlm.nih.gov/pubmed/16584128

RTI-336 was developed as a selective dopamine transporter (DAT) inhibitor. It is known that DAT inhibitors have been developed as a promising treatment approach for cocaine dependence. RTI-336 can be a useful adjunct in the treatment of cocaine dependence because preclinical data has shown that this drug inhibits DAT with a slower onset and offset rate than cocaine and with less abuse potential and psychomotor stimulant activity. RTI-336 participated in phase I clinical trial where it showed the excellent safety and tolerability, and thus further studies in humans are warranted.

Approval Year

PubMed

Title	Date	PubMed
Effects of dopamine transporter selective 3-phenyltropane analogs on locomotor activity, drug discrimination, and cocaine self-administration after oral administration.	2006 Dec 28	17067572
Development of the dopamine transporter selective RTI-336 as a pharmacotherapy for cocaine abuse.	2006 Mar 24	16584128
A Double-Blind, Placebo-Controlled Trial Demonstrating the Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of RTI-336.	2018	30042675

Sample Use Guides

In Vivo Use Guide

RTI-336 drug product is formulated as hard, white, gelatin capsules. The dosage levels are 0.3, 1.0, and 3.0 mg (Cohort 1) and 6.0, 12.0, and 20.0 mg (Cohort 2). Subjects will receive a single dose of the study drug on study day 1.

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Fri Dec 15 18:46:25 UTC 2023` Edited by `admin` on `Fri Dec 15 18:46:25 UTC 2023`
Record UNII	8QGL4KK64H
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RTI-336 FREE BASE

Common Name

English

8-AZABICYCLO(3.2.1)OCTANE, 3-(4-CHLOROPHENYL)-8-METHYL-2-(3-(4-METHYLPHENYL)-5-ISOXAZOLYL)-, (1R,2S,3S,5S)-

Systematic Name

English

Code System Code Type Description

WIKIPEDIA

RTI-336