Biological Activity
Dopamine uptake inhibitor; displays high affinity for the dopamine transporter (DAT) (Ki = 25 nM compared to 1330 and 1730 for NET and SERT respectively). Suppresses the effects of cocaine administration in a dose-dependent manner and decreases cocaine and methamphetamine self-administration in rats.
Compound Libraries
JHW 007 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 421.95 |
| Formula | C24H29F2NO.HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 202645-74-7 |
| PubChem ID | 71771746 |
| InChI Key | RHYMGBAYGRUKNZ-DHWZJIOFSA-N |
| Smiles | [H][C@@]12CC[C@@](C[C@H](OC(C4=CC=C(F)C=C4)C3=CC=C(F)C=C3)C2)([H])N1CCCC.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.19 | 100 | |
| ethanol | 42.19 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 421.95. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.37 mL | 11.85 mL | 23.7 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.74 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.37 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kristensen et al (2011) SLC6 neurotransmitter transporters: structure, function, and regulation. Pharm.Rev. 63 585 PMID:
Kopajtic et al (2010) Dopamine transporter-dependent and -independent striatal binding of the benztropine analog JHW 007, a cocaine antagonist with low abuse liability. J.Pharmacol.Exp.Ther. 335 703 PMID: 20855444
Velaquez-Sanchez et al (2010) The high affinity dopamine uptake inhibitor, JHW 007, blocks cocaine-induced reward, locomotor stimulation and sensitization. Eur.Neuropsychopharmacol. 20 501 PMID: 20413276
Hiranita et al (2014) Preclinical efficacy of N-substituted benztropine analogs as antagonists of methamphetamine self-administration in rats. J.Pharmacol.Exp.Ther. 348 174 PMID: 24194527
Keywords: JHW 007 hydrochloride, supplier, JHW007, dopamine, uptake, inhibitors, inhibits, DAT, transporter, Dopamine, Transporters, Dopamine, Transporters, Tocris Bioscience
