Drug intelligence / Profile preview

5-BDBD

Development stage
Preclinical
Modality
Small Molecules
Administration
Intracerebroventricular, Intrahippocampal, Intracisternal, Intraperitoneal, Intra-arterial, In Vitro
01

Overview

**5-BDBD** is a research-stage **small-molecule purinergic P2X4 receptor antagonist** widely used as a pharmacological tool to inhibit ATP-gated P2X4 ion channel signaling in cell and animal studies. Across the cited literature, it is used to suppress P2X4-dependent calcium influx, microglial activation, neuroinflammation, inflammasome signaling, and related downstream effects in models of pain, depression, traumatic brain injury, autoimmune hepatitis, asthma-associated vagal hypertonia, endometriosis, cancer signaling, and plasma-cell biology. The compound appears to function as a relatively selective P2X4 blocker in many systems, although recent comparative pharmacology studies emphasize important species differences, including weak or absent antagonism at mouse P2X4 in some assay systems. There is no evidence in the provided material that 5-BDBD is an approved therapeutic product; rather, it is best characterized as an experimental P2X4 probe compound and lead-like antagonist for target validation.

Other names
5-(3-bromophenyl)-1,3-dihydro-2H-benzofuro[3,2-e]-1,4-diazepin-2-one
02

Targets

P2RX1 (Purinergic receptor P2X 1)P2X3 (P2X purinoceptor 3)P2RX4 (P2X Purinoceptor 4)

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