[CAS NO. 112960-16-4] PD128907 HCl

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PRODUCTS SPECIFICATIONS [112960-16-4]

Catalog

SLK-S2168

Brand

Selleck

CAS

112960-16-4

DESCRIPTION [112960-16-4]

Overview

MDL	MFCD06858201
Molecular Weight	285.77
Molecular Formula	C14H19NO3.HCl
SMILES	OC1=CC([C@@]2([H])OCCN(CCC)[C@]2([H])CO3)=C3C=C1.[H]Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	3.4993 mL	17.4966 mL	34.9932 mL
5 mM	0.6999 mL	3.4993 mL	6.9986 mL
10 mM	0.3499 mL	1.7497 mL	3.4993 mL
50 mM	-	-	-

Description

PD 128907 HCl is a potent and selective agonist, with of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor.

Targets

D3 receptor ^[1]

0.64 nM(EC50)

In vitro

PD 128907 HCl is a potent and selective dopamine D3 receptor agonist, with EC50 of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor. When using [H]spiperone as the radioligand in CHOKl-cells, PD 128907 exhibits about a l000-fold selectivity for human D3 receptors (K, 1 nM) versus human D2 receptors (K, 1183 nM) and a l0000-fold selectivity versus human D4receptors (K, 7000 nM) PD 128907 is used for studying the role of these receptors in the brain, in roles such as inhibitory autoreceptors that act to limit further dopamine release.

In vivo

PD 128907 is active in reducing DA synthesis both in normal and γ-butyrolactone (GBL) treated rats. PD 128907 (3 mg/kg) reduces toxicity from cocaine overdose, completely prevented the convulsant and lethal effects of cocaine. The protection occurs through a D3-linked mechanism and that protection is extended to seizure kindling.

References

[1] Sautel F, et al. Neuroreport, 1995, 6(2), 329-332.
[2] Akunne HC, et al. Life Sci, 1995, 57(15), 1401-1410.
[3] Koeltzow TE, et al. J Neurosci, 1998, 18(6), 2231-2238.
[4] Pugsley TA, et al. J Pharmacol Exp Ther, 1995, 275(3), 1355-1366.
[5] Witkin JM, et al. J Pharmacol Exp Ther, 2004, 308(3):957-64.
[6] Witkin JM, et al. J Pharmacol Exp Ther, 2008, 326(3), 930-938.