AI Article Synopsis
- Selective estrogen receptor β (ERβ) agonists like AC-186 may be safer alternatives to nonselective estrogens used in hormone replacement therapy, as they primarily activate ERβ.
- In a rat model of Parkinson's disease, AC-186 demonstrated neuroprotective effects by preventing motor and cognitive deficits and protecting dopamine neurons, but these benefits were only observed in males.
- Unlike 17β-estradiol, which activates both ERβ and ERα, AC-186 provided stronger neuroprotection in male rats, indicating a unique advantage for selective ERβ activation.
Article Abstract
Drugs that selectively activate estrogen receptor β (ERβ) are potentially safer than the nonselective estrogens currently used in hormonal replacement treatments that activate both ERβ and ERα. The selective ERβ agonist AC-186 was evaluated in a rat model of Parkinson's disease induced through bilateral 6-hydroxydopamine lesions of the substantia nigra. In this model, AC-186 prevented motor, cognitive, and sensorimotor gating deficits and mitigated the loss of dopamine neurons in the substantia nigra, in males, but not in females. Furthermore, in male rats, 17β-estradiol, which activates ERβ and ERα with equal potency, did not show the same neuroprotective benefits as AC-186. Hence, in addition to a beneficial safety profile for use in both males and females, a selective ERβ agonist has a differentiated pharmacological profile compared to 17β-estradiol in males.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3778431 | PMC |
| http://dx.doi.org/10.1021/cn400132u | DOI Listing |
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