Saclofen是一种口服竞争性GABAB受体拮抗剂，IC50值为7.8µM。
Cas No.:125464-42-8
Sample solution is provided at 25 µL, 10mM.
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Saclofen is an orally competitive GABAB receptor antagonist, with an IC50 value of 7.8µM[1]. Saclofen attenuates the reduction of NO2-and NO3- without affecting nitric oxide (NO) releases in the rat striatum [2]. Saclofen is widely used to inhibit μ opioid agonist-induced feeding elicited from the nucleus accumbens shell in rats [3].
In vitro, Saclofen treatment at 100µM for 2 days regulated the migration of bromodeoxyuridine (BrdU)-positive rat cortical cells, resulting in the occurrence of cell aggregation[4].
In vivo, Saclofen treatment at a single dose of 50μg/10μl/rat (i.c.) for 60 minutes reduced the increase of serum TNF-α and IL-6 induced by lipopolysaccharide (LPS), and alleviated the inflammatory response in rats[5]. Five minutes before the injection of zymosan (30μg), intrathecal administration of Saclofen (1μg/5μl) significantly reduced the formation of knee joint edema in mice, and reduced the intra-articular levels of TNF-α and IL-1β[6].
References:
[1] Drew C A, Johnston G A R, Kerr D I B, et al. Inhibition of baclofen binding to rat cerebellar membranes by phaclofen, saclofen, 3-aminopropylphosphonic acid and related GABAB receptor antagonists[J]. Neuroscience letters, 1990, 113(1): 107-110.
[2] Adachi Y U, Kimura-Kuroiwa K, Kobayashi A, et al. The propofol-induced inhibition of nitric oxide release in rats brain was antagonized by perfusion of saclofen, GABAB receptor antagonist, using in vivo microdialysis experiment: 7AP4-8[J]. European Journal of Anaesthesiology| EJA, 2011, 28: 105.
[3] Znamensky V, Echo J A, Lamonte N, et al. γ-Aminobutyric acid receptor subtype antagonists differentially alter opioid-induced feeding in the shell region of the nucleus accumbens in rats[J]. Brain research, 2001, 906(1-2): 84-91.
[4] Behar T N, Schaffner A E, Scott C A, et al. GABA receptor antagonists modulate postmitotic cell migration in slice cultures of embryonic rat cortex[J]. Cerebral Cortex, 2000, 10(9): 899-909.
[5] Sallam M Y, El-Gowilly S M, Abdel-Galil A G A, et al. Central GABAA receptors are involved in inflammatory and cardiovascular consequences of endotoxemia in conscious rats[J]. Naunyn-Schmiedeberg's archives of pharmacology, 2016, 389(3): 279-288.
[6] Bassi G S, do C. Malvar D, Cunha T M, et al. Spinal GABA-B receptor modulates neutrophil recruitment to the knee joint in zymosan-induced arthritis[J]. Naunyn-Schmiedeberg's archives of pharmacology, 2016, 389(8): 851-861.
Saclofen是一种口服竞争性GABAB受体拮抗剂，IC50值为7.8µM[1]。Saclofen能减轻大鼠纹状体中NO2-和NO3-的减少，而不影响一氧化氮（NO）的释放[2]。Saclofen被广泛用于抑制大鼠伏隔核壳区μ阿片受体激动剂诱导的进食行为[3]。
在体外，使用100µM的Saclofen处理2天，调节了溴脱氧尿苷（BrdU）阳性大鼠皮层细胞的迁移，导致细胞聚集的发生[4]。
在体内，单次给予50µg/10µl/只大鼠（脑室内注射）剂量的Saclofen处理60分钟，降低了脂多糖（LPS）诱导的血清TNF-α和IL-6的升高，并减轻了大鼠的炎症反应[5]。在注射酵母聚糖（30µg）前5分钟，鞘内给予Saclofen（1µg/5µl）显著减少了小鼠膝关节水肿的形成，并降低了关节腔内TNF-α和IL-1β的水平[6]。
| Animal experiment [1]: | |
Animal models | Male Balb/c mice |
Preparation Method | Adult male Balb/c mice (22-26g) were housed in a room with a temperature controlled at 22±1°C and maintained in a 12-hour light/12-hour dark circadian rhythm. Under light-induced isoflurane anesthesia (1.5%), 10μl of Zymosan suspension (3μg/μl; dissolved in sterile normal saline) was injected into the tibiofemoral joint of the mice's knees to establish the arthritis model. Five minutes before intramuscular injection of Zymosan (30μg), the intrathecal administration of Saclofen (1μg/5μl) was performed, and the inflammatory factors in the joint fluid were analyzed. |
Dosage form | 1μg/5μl for once; i.t. |
Applications | Saclofen treatment significantly reduced the intra-articular levels of TNF-α and IL-1β in mice. |
References: | |
| Cas No. | 125464-42-8 | SDF | |
| 别名 | 3-氨基-2-(4-氯苯基-丙烷磺酸 | ||
| 化学名 | (R)-3-amino-2-(4-chlorophenyl)propane-1-sulfonic acid | ||
| Canonical SMILES | ClC1=CC=C(C=C1)[C@H](CN)CS(O)(=O)=O | ||
| 分子式 | C9H12ClNO3S | 分子量 | 249.72 |
| 溶解度 | 0.1 M NaOH: 10 mg/ml; DMSO: 0.3 mg/ml | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0045 mL | 20.0224 mL | 40.0449 mL |
| 5 mM | 800.9 μL | 4.0045 mL | 8.009 mL |
| 10 mM | 400.4 μL | 2.0022 mL | 4.0045 mL |
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