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  • BTS 54-505 hydrochloride
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BTS 54-505 hydrochloride

Potent SNRI,sibutramine metabolite

原价
¥425-5762
价格
340-4610
BTS 54-505 hydrochloride的二维码

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  • 库存: 现货
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  • 货号: ajci7010
  • CAS: 84484-78-6
  • 别名: 1-[1-(4-氯苯基)环丁基]-3-甲基丁胺盐酸盐
  • 分子式: C15H22NCl.HCl
  • 分子量: 288.26
  • 纯度: >98%
  • 溶解度: <28.83mg/ml in DMSO; <14.41mg/ml in Water
  • 储存: Desiccate at RT
  • 库存: 现货

Background

IC50: 0.066 μM for noradrenaline uptake; 5.1 μM for 5-HT uptake; 0.31 μM for dopamine uptake


Sibutramine HCl (BTS 54-524) is an inhibitor of the reuptake of monoamines with a pharmacological profile in rodents indicative of non-tricyclic putative antidepressant activity. BTS 54-505 is the primary amine metabolite of sibutramine.


In vitro: Simultaneous application of BTS 54-505 with 5-HT resulted in a prolongation of the recovery time from the 5-HT-mediated suppression of discharge activity. BTS 54-505 also prolonged the recovery time from a NA-mediated potentiation of firing. These effects on recovery time are attributed to the inhibition of uptake of both 5-HT and NA by BTS 54-505. The amplitude of the response to 5-HT or NA was unaffected by co-ejection of BTS 54-505 [1].


In vivo: The secondary (BTS 54-354) and primary (BTS 54-505) amine metabolites of sibutramine HCl exhibit similar in vivo pharmacological activity to the parent compound. Thus, each compound displays potent activity in acute behavioural models predictive of antidepressant effects and a comparable ability to inhibit the uptake of monoamines [2].


Clinical trial: Up to now, BTS 54-505 is still in the preclinical development stage.

Reference:
[1] Scott G, Luscombe GP, Mason R.? The effects of BTS 54-505, a metabolite of sibutramine, on monoamine and excitatory amino acid-evoked responses in the rat dorsolateral geniculate nucleus in vivo. Br J Pharmacol. 1994 Jan;111(1):97-102.
[2] Luscombe GP, Hopcroft RH, Thomas PC, Buckett WR.? The contribution of metabolites to the rapid and potent down-regulation of rat cortical beta-adrenoceptors by the putative antidepressant sibutramine hydrochloride. Neuropharmacology. 1989 Feb;28(2):129-34.

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