Pyrilamine maleate (Mepyramine), Histamine receptor H1 inverse agonist; Sequesters G(q/11) (TBI3108)

Description

Product Details

Formal Name: (S)-α-Cyano-3-phenoxybenzyl (1R, 3R)-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate

Molecular Formula: C₂₂H₁₉Br₂NO₃

Formula Weight: 505.20

CAS Number: 59-33-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DSMO (up to 50 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Histamine receptor H1 inverse agonist; Sequesters G(q/11)

Functions

Reported to be an inhibitor of calcineurin (PP2B), IC50~100 pM but this activity has been disputed. Markedly enhances the expression of BDNF in cultured rat cortical neurons and displays neurotrophic effects. Produces antidepressant-like effects in mice. Blocks the spontaneous down-regulation of Nav1.8 sodium channels expressed in Xenopus oocytes.

Application Procedures

First dissolved in DSMO (up to 50 mg/ml), then diluted to aqueous buffer.