CGP 25454A
Cat. No. :YN1730004
CAS No. :104391-26-6
86-020-82000279
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order@ubiochem.com| Product Name: | CGP 25454A |
| CAS NO.: | 104391-26-6 |
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| Molecular Weight: | 346.25 |
| Molecular Formula: | C₁₅H₂₁Cl₂N₃O₂ |
| SMILES: | O=C(NCCN(CC)CC)C1=CC(C#N)=C(Cl)C=C1OC.[H]Cl |
| Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Transportation: | Room temperature in continental US; may vary elsewhere. |
| Description: | CGP 25454A is a novel and selective presynaptic dopamine autoreceptor antagonist. In vitro: CGP 25454A increase the field-stimulated [3H]- and [14C]-overflow from rat striatal slices preloaded with [3H]dopamine and [14C]choline, indicating that CGP 25454A is able to enhance the release of both dopamine (DA) and acetylcholine (ACh). However, CGP 25454A is 12.9 times more potent in increasing, by 1/6 of the apparent maximal increase, the release of [3H]DA than that of [14C]ACh. In vivo: CGP 25454A increase [3H]spiperone binding to receptors of the D2 family in rat striatum by 90-110% (ED50: 13 mg/kg i.p.). As a similar increase in [3H]spiperone binding is found with a variety of agents which increase the synaptic concentration of endogenous DA, the effect of CGP 25454A most probably reflects an enhanced release of DA under in vivo conditions. At 30-100 mg/kg, CGP 25454A inhibit [3H]spiperone binding in the pituitary of the same animals as a result of a blockade of postsynaptic DA receptors. |
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