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Tian, Gui-Long ; Hsieh, Chia-Ju ; Taylor, Michelle , et al. Eur. J. Med. Chem.,2023,261,115751. DOI: 10.1016/j.ejmech.2023.115751 PubMed ID: 37688938
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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
Purchased from AmBeed: 89031-84-5 ; 40216-83-9 ; 88-13-1 ; 135042-17-0 ; 110-52-1 ; 488-93-7 ; 18742-02-4 ; 98-98-6 ; 86864-60-0 ; 62-23-7 ; 29886-64-4 ; 59741-04-7 ; 4385-62-0 ; 15268-31-2 ; 134441-72-8 ; 54751-01-8 ; 166173-78-0 ; 213131-32-9 ; 98-98-6 ; 69966-55-8 ; 154342-67-3 ...More
CAS No. : | 18742-02-4 | MDL No. : | MFCD00003216 |
Formula : | C5H9BrO2 | Boiling Point : | - |
Linear Structure Formula : | C3H5O2CH2CH2Br | InChI Key : | GGZQLTVZPOGLCC-UHFFFAOYSA-N |
M.W : | 181.03 | Pubchem ID : | 87776 |
Synonyms : |
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Signal Word: | Danger | Class: | 6.1 |
Precautionary Statements: | P210-P261-P264-P270-P271-P280-P301+P310+P330-P302+P352-P304+P340+P312-P305+P351+P338-P332+P313-P337+P313-P370+P378-P403+P233-P403+P235-P405-P501 | UN#: | 2810 |
Hazard Statements: | H227-H301-H315-H319-H335 | Packing Group: | Ⅲ |
GHS Pictogram: |
* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.
Yield | Reaction Conditions | Operation in experiment |
---|---|---|
73% | In ethanol; toluene; | A) 2-(2-Aminoethyl)-1,3-dioxolane A suspension of 50 g of 2-(2-bromoethyl)-1,3-dioxolane (product known in literature, CAS RN = 5754-35-8) (0.27 mL, 32.5 mol), 62.5 g of potassium phthalimide (0.34 mol), 9.16 g of Bu4N+HSO4- (0.027 mol) in 150 ml of toluene was heated to 100C and under N2 stream for 3 h. After cooling to room temperature, the mixture was filtered and evaporated to dryness. By crystallization of the residue from abs. EtOH the phthalimido derivative was obtained. A solution of 58.5 g of NH2NH2.H2O (1.17 ml; 56.8 mol), 64.36 g of phthalimido derivative (0.26 mol) in 2 l of abs. EtOH was heated to reflux under N2 stream for 2.5 h. After cooling to 0C, the precipitated phthalhydrazide was filtered through a sintered funnel. By evaporation of the filtrate to dryness, 23.26 g of the desired product (0.198 mol) were obtained. Yield: 73% The 1H-NMR, 13C-NMR, IR and MS spectra are consistent with the indicated structure. |
Yield | Reaction Conditions | Operation in experiment |
---|---|---|
86% | With dichloro bis(acetonitrile) palladium(II); potassium hydrogencarbonate; norbornene; In N,N-dimethyl acetamide; water; at 70℃; for 14h;Schlenk technique; Inert atmosphere; | General procedure: A 50-mL Schlenk flask equipped with a magnetic stirring bar and a rubber septum was charged with 1H-indole substrate 1 (1.00 mmol), norbornene (188 mg, 2.00 mmol), the base [K2CO3 (276 mg, 2.00mmol), KHCO3 (300 mg, 3.00 mmol), or K2HPO4 (522 mg, 3.00mmol) as indicated], and PdCl2(MeCN)2 (25.9 mg, 0.100 mmol). A 0.5 M solution of H2O in DMA (5 mL) was added. The alkyl bromide 2 (2.00 mmol) was then added from a syringe, and the resulting mixture was degassed by three freeze-pump-thaw cycles with liquid nitrogen under high vacuum. The flask was then placed in an oil bath preheated to 70 C or 90 C, as indicated, and the mixture was stirred vigorously under balloon pressure of argon. Upon completion of the reaction (TLC), the mixture was cooled to r.t., diluted with Et2O (30 mL), and filtered. The filtrate was concentrated in arotary evaporator (60 C water bath, 8-10 mbar) to remove the Et2O and most of the DMA. The residue was purified directly by flash column chromatography [silica gel (dry loading)] to give the alkylation product 3. |
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