Phenyltoloxamine_product_DataBase

Bioactivity	Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM)[1][2][3].
Invitro	Phenyltoloxamine (10-50 μM, 24 h) demonstrates cytotoxicity in EVSA-T cells[2].Phenyltoloxamine exhibits potent Sigma 1 Receptor (S1R) binding affinity with a Ki value of 160 nM[3].Phenyltoloxamine (100 μM) inhibits human liver macrosaml CYP2D6 enzyme by 99.0%[4].
Name	Phenyltoloxamine
CAS	92-12-6
Formula	C17H21NO
Molar Mass	255.35
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Justin B.Hoekstra. Pharmacological Properties of a New Antihistaminic Agent, Phenyltoloxamine (Bristamin). Journal of the American Pharmaceutical Association (Scientific ed.). 1953, 42 (10), 587-593. [2]. Brandes LJ, et al. Evidence that the antiestrogen binding site is a histamine or histamine-like receptor. Biochem Biophys Res Commun. 1985 Jan 31;126(2):905-10. [3]. Youyi Peng, et al. Comprehensive 3D-QSAR Model Predicts Binding Affinity of Structurally Diverse Sigma 1 Receptor Ligands. J Chem Inf Model. 2019 Jan 28;59(1):486-497. [4]. Sellers, et al. Use of inhibitors of CYP2D6 enzyme for the prevention of drug abuse. Patent, US6124282.

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