Drug intelligence / Profile preview

BMS-191011

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Topical (local Application Over Dura)
01

Overview

BMS-191011 is a **synthetic small molecule** activator (opener) of the **large-conductance calcium-activated potassium channel (BKCa, also known as KCa1.1)**[1][3][5][7][10][11]. It is classified as a 1,3,4-oxadiazole derivative originally developed for therapeutic use primarily in **stroke** models and has shown **neuroprotective effects** in multiple preclinical animal models, including middle cerebral artery occlusion (MCAO) in rats[3][5][7][10][11]. BMS-191011 demonstrates high brain-availability, high affinity, and selectivity for the BKCa channel[2][4]. Beyond stroke, it has been investigated for the treatment of **salicylate-induced tinnitus** in animal models and shown to reduce behavioral manifestations associated with tinnitus via modulation of BKCa channels in auditory regions of the central nervous system[2][4]. Its mechanism involves activation (opening) of BKCa channels, which regulates cellular electrical activity, vascular tone, and neuronal excitability[9][12]. Other identified activities include dilation of retinal arterioles through BKCa activation in vivo[9][12], and modulation of platelet function in vitro[8]. BMS-191011 was developed by Bristol Myers Squibb.

Brand names
BMS-191011BMS191011BMS 191011
Other names
BMS-191011BMS191011BMS 191011BMS-A
02

Targets

KCNMA1 (Calcium-activated potassium channel subfamily M alpha member 1)

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