Phenyltoloxamine

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].

Product Specifications

CAS Number

[92-12-6]

Product Name Alternative

Bistrimin; Histionex

UNSPSC

12352005

Hazard Statement

H302

Target

Cytochrome P450; Histamine Receptor; Sigma Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/phenyltoloxamine.html

Solubility

10 mM in DMSO

Smiles

CN(C)CCOC1=CC=CC=C1CC2=CC=CC=C2

Molecular Formula

C17H21NO

Molecular Weight

255.35

Precautions

P264-P270-P330-P501

References & Citations

[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.