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Cat. No.: HY-103518

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CGP36216

CGP36216 is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a K_i value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders.

For research use only. We do not sell to patients.

CAS No.: 123691-29-2
Formula: C₅H₁₄NO₂P
Molecular Weight:151.14

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

CGP36216 Chemical Structure

CAS No.: 123691-29-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

GABAB receptor^[1]

In Vitro

CGP36216 is ineffective at GABA postsynaptic receptors, it is appreciably more active at presynaptic receptors^[2].
CGP36216 (100 µM) could increase the frequency of spontaneous firing in VTA-DA neurons^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Animal Model:

Rats^[3].
Dosage:

20 μg/Rat.
Administration:

Intra-VTA injection (ventral tegmental area).
Result:

Abolishes CPP induced by intra-VTA injection of morphine.

Chemical Information

CAS No. 123691-29-2
Molecular Weight 151.14
Formula C₅H₁₄NO₂P
SMILES

O=P(CC)(CCCN)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. William Howson, et al. Biological activity of 3-aminopropyl (methyl) phosphinic acid, a potent and selective GABAB agonist with CNS activity. Bioorganic & Medicinal Chemistry Letters. Volume 3, Issue 4, April 1993, Pages 515-518.

[2]. J Ong, et al. CGP 36216 is a selective antagonist at GABA(B) presynaptic receptors in rat brain. Eur J Pharmacol. 2001 Mar;415(2-3):191-5. [Content Brief]

[3]. Ming Chen, et al. Morphine disinhibits glutamatergic input to VTA dopamine neurons and promotes dopamine neuron excitation. Elife. 2015 Jul 24:4:e09275. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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