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Reboxetine mesylate

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Chemical Structure| 98769-84-7 同义名 : 瑞波西汀甲磺酸盐 ;PNU155950E mesylate;FCE20124 mesylate;DSSTox_GSID_45690;DSSTox_RID_81062;DSSTox_CID_25690;AC1Q6WCV;AC1L2RIX;Vestra (TN);Edronax;Reboxetine mesilate;PNU 155950E;FCE 20124;Reboxetine (mesylate)
CAS号 : 98769-84-7
货号 : A286402
分子式 : C20H27NO6S
纯度 : 99+%
分子量 : 409.497
MDL号 : MFCD18711354
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(293.04 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(122.1 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Reboxetine Mesylate is a selective noradrenaline reuptake inhibitor (NaRI), the first drug of a new antidepressant class[3]. It has a superior pharmacological selectivity to existing tricyclic antidepressants and selective serotonin reuptake inhibitors when tested in a large number of in vitro and in vivo systems[4]. The primary route of reboxetine elimination appears to be through hepatic metabolism. Less than 10% of the dose is cleared renally. A number of metabolites formed through hepatic oxidation have been identified, but reboxetine is the major circulating species in plasma. In vitro studies show that reboxetine is predominantly metabolised by cytochrome P450 (CYP) 3A4; CYP2D6 is not involved. Ketoconazole decreases the clearance of reboxetine, so that the dosage of reboxetine may need to be reduced when potent inhibitors of CYP3A4 are coadministered[5]. Moreover, the antihyperalgesic and antiallodynic effects of reboxetine are mediated by the catecholaminergic system; β2-adrenoceptors; D1-, D2/D3-dopaminergic receptors; and δ-opioid receptors. This analgesic effect of reboxetine, besides its neutral profile on glycemic control, may be advantageous in the pharmacotherapy of diabetic neuropathy-induced pain[6]. Reboxetine was well tolerated during the acute and long-term treatment phase; side-effects such as increased sweating, constipation and dry mouth were the most prominent to be reported[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.42mL

4.88mL

2.44mL
参考文献

[1]Versiani M, Cassano G, et al. Reboxetine, a selective norepinephrine reuptake inhibitor, is an effective and well-tolerated treatment for panic disorder. J Clin Psychiatry. 2002 Jan;63(1):31-7.

[2]Wong EH, Sonders MS, et al. Reboxetine: a pharmacologically potent, selective, and specific norepinephrine reuptake inhibitor. Biol Psychiatry. 2000 May 1;47(9):818-29.

[3]Sepede G, Corbo M, Fiori F, Martinotti G. Reboxetine in clinical practice: a review. Clin Ter. 2012 Jul;163(4):e255-62

[4]Wong EH, Sonders MS, Amara SG, Tinholt PM, Piercey MF, Hoffmann WP, Hyslop DK, Franklin S, Porsolt RD, Bonsignori A, Carfagna N, McArthur RA. Reboxetine: a pharmacologically potent, selective, and specific norepinephrine reuptake inhibitor. Biol Psychiatry. 2000 May 1;47(9):818-29

[5]Fleishaker JC. Clinical pharmacokinetics of reboxetine, a selective norepinephrine reuptake inhibitor for the treatment of patients with depression. Clin Pharmacokinet. 2000 Dec;39(6):413-27

[6]Turan Yücel N, Can ÖD, Demir Özkay Ü. Catecholaminergic and opioidergic system mediated effects of reboxetine on diabetic neuropathic pain. Psychopharmacology (Berl). 2020 Apr;237(4):1131-1145

[7]Kasper S, el Giamal N, Hilger E. Reboxetine: the first selective noradrenaline re-uptake inhibitor. Expert Opin Pharmacother. 2000 May;1(4):771-82