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Promethazine (hydrochloride) (CAS 58-33-3) LS-H127

Histamine H1 receptor antagonist
LS-H127-10 / 10 g / $175
LS-H127-25 / 25 g / $185
USA Shipment Only
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Description: Promethazine is a first generation histamine H1 receptor antagonist (Ki = 2.6 nM) whose antihistamine activity has been reported in guinea pigs and mice at ED50 values of 0.43 and 5.9 mg/kg, respectively. Promethazine can penetrate the CNS, depressing central H1 receptor activity, which may relate to its sedative properties, and can also inhibit muscarinic acetylcholine receptors (Ki = 22 nM). Furthermore, 32 mg/kg promethazine demonstrates antiemetic effects in ferret models of motion sickness or chemotherapy-induced nausea. H127_ChemicalStructureImage.png
N,N,α-trimethyl-10H-phenothiazine-10-ethanamine, monohydrochloride
Diprazin
Fellozine
Lergigan
Phenergan
Romergan
biochemical, chemical, antagonist
LS-H127
58-33-3
C17H20N2S • HCl
≥95%
A crystalline solid
 
CC(N(C)C)CN1C2=C(C=CC=C2)SC3=CC=CC=C31.Cl
InChI=1S/C17H20N2S.ClH/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19;/h4-11,13H,12H2,1-3H3;1H
XXPDBLUZJRXNNZ-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: HRH1 / Histamine H1 Receptor related products

Usage Information

Promethazine (hydrochloride) is supplied as a crystalline solid. A stock solution may be made by dissolving the promethazine (hydrochloride) in the solvent of choice. Promethazine (hydrochloride) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of promethazine (hydrochloride) in these solvents is approximately 2, 5, and 10 mg/ml, respectively. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of promethazine (hydrochloride) can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of promethazine (hydrochloride) in PBS, pH 7.2, is approximately 2 mg/ml. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Kubo, N., Shirakawa, S., Kuno, T., et al. Antimuscarinic effects of antihistamines: Quantitative evaluation by receptorbinding assay. Jpn. J. Pharmacol. 43(3), 277-282 (1987).
  2. Barnett, A., Iorio, L.C., Kreutner, W., et al. Evaluation of the CNS properties of SCH 29851, a potential non-sedating antihistamine. Agents Actions 43(3-4), 149-156 (1994).
  3. Nakayama, H., Yamakuni, H., Higaki, M., et al. Antiemetic activity of FK1052, a 5-HT3- and 5-HT4-receptor antagonist, in Suncus murinus and ferrets. J. Pharmacol. Sci. 98(4), 396-403 (2005).

 


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