Drug intelligence / Profile preview

SB258585

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Not Clinically Used; Research Use Only (typical Administration In Animal Studies: Intracerebroventricular, Intrahippocampal, Not Developed For Human Administration)
01

Overview

SB258585 is a **potent and selective small molecule antagonist of the serotonin 5-HT6 receptor**, demonstrating more than 100-fold selectivity for 5-HT6 over other serotonin receptor subtypes[1][10][7][12][14]. It has been used extensively as a radioligand and a pharmacological tool in neuroscience research to characterize 5-HT6 receptor binding and biological functions, including studies in animal models evaluating its impact on cognition, memory, anxiety-like and antidepressant-like behaviors, and food motivation[2][3][6][9][10]. Mechanistically, SB258585 binds with high affinity to the orthosteric site of the 5-HT6 receptor and acts as a receptor antagonist[10]. It has been researched for potential neuroprotective effects in experimental models of Alzheimer's disease, showing improvement in cognition and reduction in hippocampal apoptosis[2]. SB258585 is for **laboratory research use** only, not approved for clinical use in humans[1][4][12].

Other names
SB-258585SB258585SB 258585SB 258585 hydrochlorideSB258585 hydrochlorideSB-258585 hydrochloride
02

Targets

HTR6 (5-hydroxytryptamine receptor 6)

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