Home Cart Sign in  
Chemical Structure| 154342-67-3 Chemical Structure| 154342-67-3

Structure of 154342-67-3

Chemical Structure| 154342-67-3

*Storage: .

*Shipping: Normal

(2S,4R)-Methyl 1-ethyl-4-hydroxypyrrolidine-2-carboxylate

CAS No.: 154342-67-3

,97%

4.5 *For Research Use Only !

Cat. No.: A968168 Purity: 97%

Change View

Size Price

US Stock

Global Stock

In Stock

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

    In Stock

    - +

    US Stock: ship in 0-1 business day
    Global Stock: ship in 2 weeks

    • 1-2 Day Shipping
    • High Quality
    • Technical Support
    Product Citations

    Product Citations

    Tian, Gui-Long ; Hsieh, Chia-Ju ; Taylor, Michelle ; Lee, Ji Youn ; Riad, Aladdin A. ; Luedtke, Robert R. , et al.

    Abstract: The difference in the secondary binding site (SBS) between the dopamine 2 receptor (D2R) and dopamine 3 receptor (D3R) has been used in the design of compounds displaying selectivity for the D3R versus D2R. In the current study, a series of bitopic ligands based on Fallypride were prepared with various secondary binding fragments (SBFs) as a means of improving the selectivity of this benzamide analog for D3R versus D2R. We observed that compounds having a small alkyl group with a heteroatom led to an improvement in D3R versus D2R selectivity. Increasing the steric bulk in the SBF increase the distance between the pyrrolidine N and Asp110, thereby reducing D3R affinity. The best-in-series compound was (2S,4R)-trans-27 which had a modest selectivity for D3R versus D2R and a high potency in the β-arrestin competition assay which provides a measure of the ability of the compound to compete with endogenous dopamine for binding to the D3R. The results of this study identified factors one should consider when designing bitopic ligands based on Fallypride displaying an improved affinity for D3R versus D2R.

    Keywords: Dopamine 2 receptor ; Dopamine 3 receptor ; Fallypride ; Bitopic ligands ; PET imaging

    Alternative Products

    Product Details of [ 154342-67-3 ]

    CAS No. :154342-67-3
    Formula : C8H15NO3
    M.W : 173.21
    SMILES Code : O=C(OC)[C@H]1N(CC)C[C@H](O)C1

    Safety of [ 154342-67-3 ]

     

    Historical Records