SNAP 398299是一种galanin-3受体（Gal3）选择性拮抗剂。
Cas No.:903878-06-8
Sample solution is provided at 25 µL, 10mM.
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SNAP 398299 is a selective antagonist of the galanin-3 receptor (Gal3)[1-2]. SNAP 398299 is used in research related to anxiety and depression[3-4].
In vitro, HEK-293 cells co-expressing the human Gal3 receptor and Gαz protein were treated with SNAP 398299 (10nM-10μM) for 20 minutes, followed by incubation with 20μM Forskolin for 5 minutes. SNAP 398299 antagonized, in a concentration-dependent manner, the inhibitory effect of galanin on forskolin-stimulated adenylyl cyclase activity[5].
In vivo, rats were treated with an acute intraperitoneal injection of SNAP 398299 (1-10mg/kg) 1-2 hours prior to testing. SNAP 398299 significantly increased active social interaction time in rats, decreased immobility time, and increased swimming time in the forced swim test[5].
References:
[1] Seshan G, Kanagasabai S, Ananthasri S, et al. Insights of structure-based pharmacophore studies and inhibitor design against Gal3 receptor through molecular dynamics simulations. J Biomol Struct Dyn. 2021 Nov;39(18):6987-6999.
[2] Kothandan G, Gadhe CG, Cho SJ. Theoretical characterization of galanin receptor type 3 (Gal3 ) and its interaction with agonist (GALANIN) and antagonists (SNAP 37889 and SNAP 398299): an in silico analysis. Chem Biol Drug Des. 2013 Jun;81(6):757-74.
[3] Ogren SO, Kuteeva E, Hökfelt T, et al. Galanin receptor antagonists : a potential novel pharmacological treatment for mood disorders. CNS Drugs. 2006;20(8):633-54.
[4] Scheller KJ, Williams SJ, Lawrence AJ, et al. An improved method to prepare an injectable microemulsion of the galanin-receptor 3 selective antagonist, SNAP 37889, using Kolliphor(®) HS 15. MethodsX. 2014 Sep 26;1:212-6.
[5] Swanson CJ, Blackburn TP, Zhang X, et al. Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489-94.
SNAP 398299是一种galanin-3受体（Gal3）选择性拮抗剂[1-2]。SNAP 398299可用于焦虑和抑郁的相关研究[3-4]。
在体外，SNAP 398299（10-nM-10μM）处理表达人Gal3受体和Gαz蛋白的HEK-293细胞20min，随后施加20μM Forskolin孵育5min，SNAP 398299能够以浓度依赖的方式拮抗甘丙肽对腺苷酸环化酶活性的抑制[5]。
在体内，SNAP 398299（1-10mg/kg）急性腹腔注射处理大鼠1-2小时，SNAP 398299显著增强了大鼠的社交互动时间，并减少了强迫游泳测试中的不动时间、增加了游泳时间[5]。
| Cell experiment [1]: | |
Cell lines | HEK-293 cells (human embryonic kidney cell line) transiently cotransfected with the human Gal3 receptor and Gαz protein |
Preparation Method | HEK-293 cells were treated with SNAP 398299 at concentrations ranging from 10nM to 10μM for 20 minutes. Galanin (1μM) was then added, followed by incubation with 20μM Forskolin for 5 minutes. The inhibition of adenylyl cyclase activity was measured. |
Reaction Conditions | 10nM-10μM; 20min. |
Applications | SNAP 398299 antagonized, in a concentration-dependent and competitive manner, the inhibitory effect of galanin on forskolin-stimulated adenylyl cyclase activity. |
| Animal experiment [1]: | |
Animal models | Adult male Sprague-Dawley rats and infant Hartley guinea pigs |
Preparation Method | Rats received acute oral administration of SNAP 398299 (1, 3, and 10mg/kg) were tested in the forced swim test (FST) 2 hours later. Social interaction tests were conducted 1 hour after oral administration in rats, and guinea pig pups were observed for vocalizations after maternal separation following administration. |
Dosage form | 1, 3, 10mg/kg; p.o.; single administration |
Applications | Acute administration of SNAP 398299 significantly increased active social interaction time in rats, reduced anxiety-related vocalizations in guinea pig pups, and produced antidepressant-like effects in the forced swim test (FST) by decreasing immobility time and increasing swimming time. |
References: | |
| Cas No. | 903878-06-8 | SDF | |
| Canonical SMILES | O=C3/C(C2=CC=CC=C2N3C4=CC(OCCN5CCCC5)=CC=C4)=N/C1=CC=CC(C(F)(F)F)=C1 | ||
| 分子式 | C27H24F3N3O2 | 分子量 | 479.49 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0855 mL | 10.4277 mL | 20.8555 mL |
| 5 mM | 417.1 μL | 2.0855 mL | 4.1711 mL |
| 10 mM | 208.6 μL | 1.0428 mL | 2.0855 mL |
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- Purity: >98.00% Appearance: A solid
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