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Dexchlorpheniramine (maleate)

(Synonyms: 马来酸右氯苯那敏; S-(+)-Chlorpheniramine maleate salt) 目录号 : GC43427

A histamine H1 receptor antagonist

Dexchlorpheniramine (maleate) Chemical Structure

Cas No.:2438-32-6

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500mg
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1g
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Sample solution is provided at 25 µL, 10mM.

Description

Dexchlorpheniramine is a histamine H1 receptor antagonist with a pA2 value of 9.36 in guinea pig ileal tissue in vitro. [1] It inhibits the proliferation of previously sensitized, allergen-challenged peripheral blood mononuclear cells by 92% at a concentration of 4.8 µM. [2] Dexchlorpheniramine reduces noradrenaline uptake in the rat vas deferens ex vivo in response to tyramine stimulation when used at a concentration of 10 µM.[3]  In vivo, dexchlorpheniramine increases the pain threshold of mice exposed to thermal and chemical stimulation tests when administered intraperitoneally at a dose of 30 mg/kg.[4] Formulations containing dexchlorpheniramine have been used for the treatment of allergic reactions.

Reference:
[1]. Shamsa, F., Ahmadiani, A., and Khosrokhavar, R. Antihistaminic and anticholinergic activity of barberry fruit (Berberis vulgaris) in the guinea-pig ileum. J. Ethnopharmacol. 64(2), 161-166 (1999).
[2]. Holen, E., Elsayed, S., and Nyfors, A. The effect of H1 receptor antagonists on peripheral blood mononuclear cells, adenoid cells and primary cell lines. APMIS 103(2), 98-106 (1995).
[3]. Barnett, A., Symchowicz, S., and Taber, R.I. The effects of drugs inhibiting catecholamine uptake on tyramine and noradrenaline-induced contractions of the isolated rat vas deferens. Br. J. Pharmacol. 34(3), 484-492 (1968).
[4]. Farzin, D., Asghari, L., and Nowrouzi, M. Rodent antinociception following acute treatment with different histamine receptor agonists and antagonists. Pharmacol. Biochem. Behav. 72(3), 751-760 (2002).

化学性质

Cas No. 2438-32-6 SDF
别名 马来酸右氯苯那敏; S-(+)-Chlorpheniramine maleate salt
化学名 γS-(4-chlorophenyl)-N,N-dimethyl-2-pyridinepropanamine, 2Z-butenedioate
Canonical SMILES ClC(C=C1)=CC=C1[C@H](CCN(C)C)C2=CC=CC=N2.OC(/C=C\C(O)=O)=O
分子式 C16H19ClN2•C4H4O4 分子量 390.9
溶解度 DMSO : ≥ 100 mg/mL (255.85 mM); H2O : ≥ 100 mg/mL (255.85 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.5582 mL 12.791 mL 25.582 mL
5 mM 0.5116 mL 2.5582 mL 5.1164 mL
10 mM 0.2558 mL 1.2791 mL 2.5582 mL
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