GZ-793A

Modify Date: 2024-01-09 09:45:10

GZ-793A Structure
GZ-793A structure
Common Name GZ-793A
CAS Number 1356447-90-9 Molecular Weight 464.037
Density N/A Boiling Point N/A
Molecular Formula C26H38ClNO4 Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS09
GHS09
Signal Word Warning

 Use of GZ-793A


GZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an Ki of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction[1][2][3].

 Names

Name (2R)-3-{(2R,6S)-2,6-Bis[2-(4-methoxyphenyl)ethyl]-1-piperidinyl}-1,2-propanediol hydrochloride (1:1)
Synonym More Synonyms

 GZ-793A Biological Activity

Description GZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an Ki of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction[1][2][3].
Related Catalog
Target

Ki: 0.029 µM (VMAT2)[1].

In Vivo GZ-793A (30, 60, 120 or 240 mg/kg; p.o.; once) decreases the number of METH infusions self-administered across each time interval evaluats in a dose-dependent manner[1]. GZ-793A (1-100 µM; 90 min) inhibits METH (5 µM)-evoked fractional dopamine releases[2]. Animal Model: Adult male Sprague-Dawley rats[1]. Dosage: 30, 60, 120 or 240 mg/kg Administration: Oral administration; once. Result: Decreased the number of METH infusions self-administered in a dose-dependent manner, and with an ~85% reduction at the highest dose (240 mg/kg). Decreased the METH self-administration produced by lasted at least 180 min. Animal Model: Male Sprague-Dawley rats (250–275 g; 9-week-old; 0.5 mm thick rats coronal striatal slices are used)[2]. Dosage: 1-100 µM Administration: 90 min Result: Inhibited methamphetamine-evoked dopamine released in a concentration-dependent manner.
References

[1]. Wilmouth CE, et al. Oral administration of GZ-793A, a VMAT2 inhibitor, decreases methamphetamine self-administration in rats. Pharmacol Biochem Behav. 2013 Nov;112:29-33.

[2]. Nickell JR, et al. GZ-793A inhibits the neurochemical effects of methamphetamine via a selective interaction with the vesicular monoamine transporter-2. Eur J Pharmacol. 2017 Jan 15;795:143-149.

[3]. Nickell JR, et al. The vesicular monoamine transporter-2: an important pharmacological target for the discovery of novel therapeutics to treat methamphetamine abuse. Adv Pharmacol. 2014;69:71-106.

 Chemical & Physical Properties

Molecular Formula C26H38ClNO4
Molecular Weight 464.037
Exact Mass 463.248932

 Safety Information

Symbol GHS09
GHS09
Signal Word Warning
Hazard Statements H410
Precautionary Statements P273-P501
RIDADR UN 3077 9 / PGIII

 Synonyms

(2R)-3-{(2R,6S)-2,6-Bis[2-(4-methoxyphenyl)ethyl]-1-piperidinyl}-1,2-propanediol hydrochloride (1:1)
1,2-Propanediol, 3-[(2R,6S)-2,6-bis[2-(4-methoxyphenyl)ethyl]-1-piperidinyl]-, (2R)-, hydrochloride (1:1)