Drug intelligence / Profile preview

4R-cembranoid

Development stage
Preclinical
Lead developer
University of Louisiana at Monroe
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Intraperitoneal, Intravenous, Ex Vivo (tissue/cell Culture)
01

Overview

4R-cembranoid is a naturally occurring **diterpenoid**, specifically a cembranoid isolated from tobacco leaves and flowers. It is characterized by a 14-carbon cembrane ring and has two hydroxyl groups. 4R-cembranoid is notable for its **neuroprotective** and **anti-inflammatory** properties. It has been shown in preclinical studies to protect neurons against various neurotoxic insults (such as NMDA, paraoxon, and diisopropylfluorophosphate) by modulating anti-apoptotic and anti-inflammatory signaling. Its neuroprotection is partly attributed to inhibition of nicotinic acetylcholine receptor subtypes (especially α7 and possibly α4β2 and α3β4), resulting in activation of the PI3-kinase/Akt antiapoptotic pathway. 4R-cembranoid also suppresses neuroinflammation: it inhibits glial pro-inflammatory phenotypes, decreases expression of iNOS, upregulates arginase-1, and reduces microglial/astrocyte activation markers. It can cross the blood-brain barrier rapidly and has a favorable safety profile at experimentally tested doses. Research has focused on its potential for neurodegenerative diseases such as Parkinson’s disease and conditions with neuroinflammatory components[1][2][3][4].

Other names
(1S, 2E, 4R, 6R, 7E, 11E)-2,7,11-cembratriene-4,6-diol4R cembranoid
02

Targets

CREB (Cyclic AMP response element-binding protein)STAT3 (Signal Transducer and Activator of Transcription 3)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)CHRNA7 (α7 nicotinic receptor)

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