TALIPEXOLE DIHYDROCHLORIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C10H15N3S.2ClH
Molecular Weight	282.233
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.Cl.NC1=NC2=C(CCN(CC=C)CC2)S1

InChI

InChIKey=DPQAXNSOFFYKDS-UHFFFAOYSA-N

InChI=1S/C10H15N3S.2ClH/c1-2-5-13-6-3-8-9(4-7-13)14-10(11)12-8;;/h2H,1,3-7H2,(H2,11,12);2*1H

HIDE SMILES / InChI

Description
Sources: http://link.springer.com/article/10.2165/00023210-199707050-00007
Curator's Comment: Description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/8842679

Talipexole is a D2 receptor agonist which was marketed in June 1996 in Japan for the treatment of Parkinson's disease. Clinical trials with talipexole in patients with Parkinson's disease demonstrated statistically significant improvements from baseline for parkinsonian symptoms including akinesia, rigidity, tremor and gait disturbances.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 297 Target ID: CHEMBL217 Sources: http://www.ncbi.nlm.nih.gov/pubmed/10455328	Agonist 2678	5.8 null [pKi]
Dopamine D3 receptor 91 Target ID: CHEMBL234 Sources: http://www.ncbi.nlm.nih.gov/pubmed/10455328	Agonist 2678	7.0 null [pKi]
Alpha-2a adrenergic receptor 63 Target ID: CHEMBL1867 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12388666	Agonist 2678	7.43 null [pKi]
Alpha-2b adrenergic receptor 27 Target ID: CHEMBL1942 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12388666	Agonist 2678	7.09 null [pKi]
Alpha-2c adrenergic receptor 37 Target ID: CHEMBL1916 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12388666	Agonist 2678	7.37 null [pKi]
Dopamine D4 receptor 71 Target ID: CHEMBL219 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12388666	Agonist 2678	6.48 null [pKi]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Chronic schizophrenia 6 Sources: http://www.ncbi.nlm.nih.gov/pubmed/8102551	Primary		Preclinical	Unknown Approved Use Unknown
Parkinson's disease 226 Sources: http://link.springer.com/article/10.2165/00023210-199707050-00007	Primary		Phase II 1132	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Intranasal application of the alpha2-adrenoceptor agonist BHT-920 produces decongestion in the cat.	2001 Nov-Dec	11777250
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.	2002 Nov	12388666
Practice parameters for the dopaminergic treatment of restless legs syndrome and periodic limb movement disorder.	2004 May 1	15164914
Drug treatment of Parkinson's disease.	2004 Sep	22033779
Pre-junctional alpha2-adrenoceptors modulation of the nitrergic transmission in the pig urinary bladder neck.	2007	17266136
Effect of bromocriptine on the severity of ovarian hyperstimulation syndrome and outcome in high responders undergoing assisted reproduction.	2010 May	21209752
[Dopaminergic neuroprotection and reconstruction of neural network tiara].	2010 Oct	20930477

Patents

Sample Use Guides

In Vivo Use Guide

Initially 0.2 or 0-4 mg/day, increased by 0.4 mg every week (usual maintenance dosage 1.2 to 3.6 mg/day) Below 0.8 mg/day, once a day; 0.8 to 1.2 mg/day, twice a day; over 1.2 mg/day, 3 times a day

Route of Administration: Oral

In Vitro Use Guide

Talipexole at low concentration (0.1-1 mM) significantly inhibited the accumulation of cytochrome c in the cytosolic fraction of human neuroblastoma SH-SY5Y cells

Name

Type

Language

TALIPEXOLE DIHYDROCHLORIDE

Common Name

English

TALIPEXOLE HYDROCHLORIDE

Common Name

English

TALIPEXOLE DIHYDROCHLORIDE [MI]

Common Name

English

Talipexole hydrochloride [WHO-DD]

Common Name

English

TALIPEXOLE HYDROCHLORIDE [JAN]

Common Name

English

TALIPEXOLE HYDROCHLORIDE [MART.]

Common Name

English

TALIPEXOLE HCL

Common Name

English

Code System Code Type Description

CAS

36085-73-1