Preparation of an affinity chromatography matrix for the selective purification of the dopamine D2 receptor from bovine striatal membranes was written by Clagett-Dame, Margaret;Schoenleber, Robert;Chung, Christine;McKelvy, Jeffrey F.. And the article was included in Biochimica et Biophysica Acta, Biomembranes in 1989.Formula: C12H14ClFO2 This article mentions the following:
A ligand affinity matrix has been developed and utilized to purify the dopamine D2 receptor ∼2100-fold from bovine striatal membranes. 3-[2-Aminoethyl]-8-[3-(4-fluorobenzoyl)propyl]-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (AES) was synthesized and used to prepare the affinity matrix by coupling to epoxy-activated Sepharose 6B (AES-Sepharose). AES (Ki ≈ 1.7 nM) is similar in potency to the parent compound, spiperone (Ki ≈ 0.8 mM), in competing for [3H]spiperone-binding activity. AES has no significant potency in competing for the dopamine D1 receptor as assessed by competition for [3H]SCH23390 binding (K2 > 1 μM)9. Covalent photoaffinity labeling of the dopamine D2 receptor in bovine striatal membranes with N-(p-azido-m-[125I]iodophenethyl)spiperone ([125I]N3-NAPS) was prevented by AES at nanomolar concentrations The dopamine D2 receptor was solubilized from bovine striatal membranes using 0.25% cholate in the presence of high ionic strength, followed by precipitation and subsequent treatment with 0.5% digitonin. Nearly 100% of the [3H]spiperone-binding activity in the cholate-digitonin solubilized preparation was adsorbed at a receptor-to-resin ratio of 2:1 (volume/volume). Dopamine D2 receptor was eluted from the affinity resin using a competing dopaminergic antagonist mol., haloperidol. Recovery of dopamine D2 receptor activity from the affinity matrix was ∼9% of the activity adsorbed to the resin. The [3H]spiperone-binding activity in AES-Sepharose affinity purified preparations is saturable and of high affinity (0.2 nM). Affinity-purified preparations maintain the ligand-binding characteristics of a dopamine D2 receptor as assessed by agonist and antagonist competition for [3H]spiperone binding. In the experiment, the researchers used many compounds, for example, 2-(3-Chloropropyl)-2-(4-fluorophenyl)-1,3-dioxolane (cas: 3308-94-9Formula: C12H14ClFO2).
2-(3-Chloropropyl)-2-(4-fluorophenyl)-1,3-dioxolane (cas: 3308-94-9) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. Dioxole functionalized metal-organic frameworks have also been recently reported.Formula: C12H14ClFO2
Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem