G9659
Sigma

GBR 12935 dihydrochloride

≥98% (TLC), powder

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Synonym

1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride

Molecular Formula

C₂₈H₃₄N₂O · 2HCl

Molecular Weight

487.50

CAS Number

67469-81-2

MDL number

MFCD00083175

PubChem Substance ID

24277959

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Descriptions

Biochem/physiol Actions

Inhibits the dopamine and norepinephrine transporters with K_is of 21.5 nM and 225 nM, respectively. Does not inhibit the serotonin transporter (K_i = 6.5 μM). Binds to a nondopaminergic piperazine site in blood platelets and brain that has been identified as cytochrome P450.

Properties

assay

≥98% (TLC)

form

powder

color

white

solubility

H₂O: 20 mg/mL with warming

References

Reference

Gordon, I., et al., [³H]GBR 12935 binding to human platelet membranes is sensitive to piperazine derivatives but not to dopamine uptake inhibitors. Life Sci. 55, 189-199, (1994) abstract

Akunne, H.C., et al., Studies of the biogenic amine transporters. III. Demonstration of two binding sites for [³H]GBR12935 and [³H]BTCP in rat caudate membranes. J. Pharmacol. Exp. Ther. 268, 1462-1475, (1994) abstract

Allard, P., et al., [³H]GBR-12935 binding to cytochrome P450 in the human brain. J. Neurochem. 62, 342-348, (1994) abstract

Torres, G.E., et al.
, Plasma membrane monoamine transporters: structure, regulation and function. Nat. Rev. Neurosci. 4, 13-25, (2003) abstract

Hiroi, T., et al., Specific binding of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6. Biochem. Pharmacol. 53, 1937-1939, (1997) abstract

Safety

WGK Germany