| Identification | Back Directory | [Name]
3-[(2R,6S)-2,6-Bis[2-(4-methoxyphenyl)ethyl]-1-piperidinyl]-(2R)-1,2-propanediol hydrochloride | [CAS]
1356447-90-9 | [Synonyms]
GZ-793A
GZ793A; GZ 793A
GZ-793A >=98% (HPLC)
(R)-3-[2,6-cis-Di(4-methoxyphenethyl)piperidin-1-yl]propane-1,2-diol hydrochloride
3-[(2R,6S)-2,6-Bis[2-(4-methoxyphenyl)ethyl]-1-piperidinyl]-(2R)-1,2-propanediol hydrochloride | [Molecular Formula]
C26H38ClNO4 | [MDL Number]
MFCD27952933 | [MOL File]
1356447-90-9.mol | [Molecular Weight]
464.04 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
H2O: soluble3mg/mL, clear | [form ]
powder | [color ]
white to beige | [Water Solubility ]
H2O: 3mg/mL, clear | [InChIKey]
FLFFCQKGCYZDOI-SJUVJREQSA-N | [SMILES]
Cl.N1([C@H](CCC[C@H]1CCc3ccc(cc3)OC)CCc2ccc(cc2)OC)C[C@@H](O)CO |
| Safety Data | Back Directory | [Hazard Codes ]
N | [Risk Statements ]
50/53 | [Safety Statements ]
60-61 | [RIDADR ]
UN 3077 9 / PGIII | [WGK Germany ]
3 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Aquatic Acute 1
Aquatic Chronic 1 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
GZ-793A is a selective inhibitor of vesicular monoamine transporter 2 (VMAT2)which transports the monoamine neurotransmitters from cellular cytosol into synaptic vesicles. GZ-793A is 50-fold selective for VM at over the serotonin or dopamine transporters. VMAT2 has recently been considered a target for the treatment of methamphetamine abuse. In r at studiesGZ-793A decreased self-administration of methamphetamine with no development of tolerance. | [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. DOI:10.1016/j.pbb.2013.09.006
[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. DOI:10.1016/j.ejphar.2016.12.016
[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. DOI:10.1016/B978-0-12-420118-7.00002-0 |
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| Company Name: |
Energy Chemical
|
| Telephone: |
400-0056266 |
| Website: |
www.energy-chemical.com |
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