کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2058726 | 1543969 | 2014 | 5 صفحه PDF | دانلود رایگان |

Research into the galanin-3 (GAL3) receptor has many challenges, including the lack of commercially available selective ligands. While the identification of non-peptidergic GAL3 receptor-selective antagonists, 1-phenyl-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one (SNAP 37889) and 1-[3-(2-pyrrolidin-1-ylethoxy)phenyl]-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one (SNAP 398299) have implicated a role for GAL3 receptors in anxiety, depression and drug-seeking behaviour, a major limitation of their use is poor aqueous solubility. Previously we have used 5% dimethylsulfoxide (DMSO) with 1% hydroxypropylmethyl cellulose in saline to dissolve SNAP 37889 for intraperitoneal (i.p.) injections of rats; however this produced a micro-suspension that was not ideal. The injectable formulation of SNAP 37889 was improved as follows:
• 30% (w/v) Kolliphor® HS 15 (Solutol HS® 15) and sodium phosphate buffer (0.01 M, pH 7.4) were used as vehicles.
• A smooth glass mortar and pestle was used to triturate the Kolliphor® HS 15 and SNAP 37889 into a paste before addition to the sodium phosphate buffer at room temperature (RT).
• The resulting mixture was vortexed until the paste was fully dissolved and the microemulsion was allowed to sit for 20 min to allow air bubbles to coalesce.
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Journal: MethodsX - Volume 1, 2014, Pages 212–216