CAS 145821-59-6|Tiagabine hydrochloride

Introduction：Basic information about CAS 145821-59-6|Tiagabine hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Tiagabine hydrochloride BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles2
6. Synonyms

Common Name	Tiagabine hydrochloride
CAS Number	145821-59-6	Molecular Weight	412.009
Density	/	Boiling Point	568ºC at 760 mmHg
Molecular Formula	C₂₀H₂₆ClNO₂S₂	Melting Point	>192oC dec.
MSDS	ChineseUSA	Flash Point	297.3ºC
Symbol	GHS02, GHS06, GHS08	Signal Word	Danger

Names

Name	tiagabine hydrochloride
Synonym	More Synonyms

Tiagabine hydrochloride BiologicalActivity

Description	Tiagabine hydrochloride(NO328 hydrochloride) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.Target: GABA reuptake inhibitorTiagabine had an early onset of effect, as shown by significant reduction from baseline in mean HAM-A total score compared with placebo at week 1 (observed cases, p < .05). Tiagabine was generally well tolerated and not associated with changes in sexual functioning or depressive status. Symptoms of a discontinuation syndrome during taper were not observed. Tiagabine may be a useful treatment option for adult patients diagnosed with GAD [1]. Tiagabine was generally well tolerated; the most common adverse events were nausea, dizziness and headaches [2]. Tiagabine (0.1 microM), an antiepileptic drug that specifically inhibits the GAT-1 GABA transporter inhibited GABA uptake 50% in temporal cortex and 60-68% in white structures [3].
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>GABA ReceptorSignaling Pathways >>Neuronal Signaling >>GABA ReceptorResearch Areas >>Neurological Disease
References	[1]. Pollack, M.H., et al., The selective GABA reuptake inhibitor tiagabine for the treatment of generalized anxiety disorder: results of a placebo-controlled study. J Clin Psychiatry, 2005. 66(11): p. 1401-8. [2]. Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40(3): p. 32-40. [3]. Henjum, S. and B. Hassel, High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int, 2007. 50(2): p. 365-70.

Description

Tiagabine hydrochloride(NO328 hydrochloride) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.Target: GABA reuptake inhibitorTiagabine had an early onset of effect, as shown by significant reduction from baseline in mean HAM-A total score compared with placebo at week 1 (observed cases, p < .05). Tiagabine was generally well tolerated and not associated with changes in sexual functioning or depressive status. Symptoms of a discontinuation syndrome during taper were not observed. Tiagabine may be a useful treatment option for adult patients diagnosed with GAD [1]. Tiagabine was generally well tolerated; the most common adverse events were nausea, dizziness and headaches [2]. Tiagabine (0.1 microM), an antiepileptic drug that specifically inhibits the GAT-1 GABA transporter inhibited GABA uptake 50% in temporal cortex and 60-68% in white structures [3].

Related Catalog

Signaling Pathways >>Membrane Transporter/Ion Channel >>GABA ReceptorSignaling Pathways >>Neuronal Signaling >>GABA ReceptorResearch Areas >>Neurological Disease

References

[1]. Pollack, M.H., et al., The selective GABA reuptake inhibitor tiagabine for the treatment of generalized anxiety disorder: results of a placebo-controlled study. J Clin Psychiatry, 2005. 66(11): p. 1401-8.

[2]. Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40(3): p. 32-40.

[3]. Henjum, S. and B. Hassel, High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int, 2007. 50(2): p. 365-70.

Chemical & Physical Properties

Boiling Point	568ºC at 760 mmHg
Melting Point	>192oC dec.
Molecular Formula	C₂₀H₂₆ClNO₂S₂
Molecular Weight	412.009
Flash Point	297.3ºC
Exact Mass	411.109344
PSA	97.02000
LogP	5.78470
Vapour Pressure	9.71E-14mmHg at 25°C
InChIKey	YUKARLAABCGMCN-PKLMIRHRSA-N
SMILES	Cc1ccsc1C(=CCCN1CCCC(C(=O)O)C1)c1sccc1C.Cl
Storage condition	-20°C Freezer

Safety Information

Symbol	GHS02, GHS06, GHS08
Signal Word	Danger
Hazard Statements	H225-H301 + H311 + H331-H370
Precautionary Statements	P210-P260-P280-P301 + P310-P311
Hazard Codes	Xn
Risk Phrases	R20/21/22
Safety Phrases	36/37
RIDADR	UN1230 - class 3 - PG 2 - Methanol, solution

Articles2

Behavioral and cognitive effects of anti-epileptic drugs.

Discov. Med. 9(45) , 138-44, (2010)

Anti-epileptic drugs (AEDs) have a variety of mechanisms of action which are reflected through different anticonvulsant activities and behavioral effects. Two categories of AEDs are considered based o...

A novel compound N(1),N(5)-(Z)-N(10)-(E)-tri-p-coumaroylspermidine isolated from Carthamus tinctorius L. and acting by serotonin transporter inhibition.

Eur. Neuropsychopharmacol. 19(10) , 749-58, (2009)

Safflower, the dry flower of Carthamus tinctorius L., has long been applied for empirically treating cerebral ischemia and depression in traditional Chinese medicine. Pathogenesis of major depression ...

Synonyms

(-)-(R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid hydrochloride

acide (3R)-1-[4,4-bis(3-méthylthiophén-2-yl)but-3-én-1-yl]pipéridine-3-carboxylique chlorhydrate

Abbott-70569.1

EINECS 200-659-6

(3R)-1-[4,4-Bis(3-methyl-2-thienyl)but-3-en-1-yl]piperidine-3-carboxylic acid hydrochloride (1:1)

(3R)-1-[4,4-Bis(3-methylthiophen-2-yl)but-3-en-1-yl]piperidin-3-carbonsäurehydrochlorid

3-Piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-buten-1-yl]-, (3R)-, hydrochloride (1:1)

Tiagabine hydrochloride

(3R)-1-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)-3-piperidinecarboxylic acid hydrochloride

(3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl]piperidine-3-carboxylic acid hydrochloride

(3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylic acid,hydrochloride

(3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl]piperidine-3-carboxylic acid hydrochloride (1:1)

MFCD07369025

(3R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-buten-1-yl]-3-piperidinecarboxylic acid hydrochloride (1:1)

Abbott-70569.HCl

3-piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-, (3R)-, hydrochloride

Tiagabine (hydrochloride)

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