AC-186, a Selective Nonsteroidal Estrogen Receptor beta Agonist, Shows Gender Specific Neuroprotection in a Parkinson's Disease Rat Model

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AC-186, a Selective Nonsteroidal Estrogen Receptor beta Agonist, Shows Gender Specific Neuroprotection in a Parkinson's Disease Rat Model. / McFarland, Krista; Price, Diana L.; Davis, Christopher N.; Ma, Jian-Nong; Bonhaus, Douglas W.; Burstein, Ethan S.; Olsson, Roger.

I: ACS Chemical Neuroscience, Vol. 4, Nr. 9, 2013, s. 1249-1255.

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McFarland, Krista ; Price, Diana L. ; Davis, Christopher N. ; Ma, Jian-Nong ; Bonhaus, Douglas W. ; Burstein, Ethan S. ; Olsson, Roger. / AC-186, a Selective Nonsteroidal Estrogen Receptor beta Agonist, Shows Gender Specific Neuroprotection in a Parkinson's Disease Rat Model. I: ACS Chemical Neuroscience. 2013 ; Vol. 4, Nr. 9. s. 1249-1255.

RIS

TY - JOUR

T1 - AC-186, a Selective Nonsteroidal Estrogen Receptor beta Agonist, Shows Gender Specific Neuroprotection in a Parkinson's Disease Rat Model

AU - McFarland, Krista

AU - Price, Diana L.

AU - Davis, Christopher N.

AU - Ma, Jian-Nong

AU - Bonhaus, Douglas W.

AU - Burstein, Ethan S.

AU - Olsson, Roger

PY - 2013

Y1 - 2013

N2 - Drugs that selectively activate estrogen receptor beta (ER beta) are potentially safer than the nonselective estrogens currently used in hormonal replacement treatments that activate both ER beta and ER alpha. The selective ER beta 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, 17 beta-estradiol, which activates ER beta and ER alpha 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 ER beta agonist has a differentiated pharmacological profile compared to 17 beta-estradiol in males.

AB - Drugs that selectively activate estrogen receptor beta (ER beta) are potentially safer than the nonselective estrogens currently used in hormonal replacement treatments that activate both ER beta and ER alpha. The selective ER beta 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, 17 beta-estradiol, which activates ER beta and ER alpha 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 ER beta agonist has a differentiated pharmacological profile compared to 17 beta-estradiol in males.

KW - Parkinson's disease

KW - neuroprotection

KW - AC-186

KW - gender difference

KW - buccal/sublingual administration

KW - selective estrogen receptor beta

KW - agonist

U2 - 10.1021/cn400132u

DO - 10.1021/cn400132u

M3 - Article

VL - 4

SP - 1249

EP - 1255

JO - ACS Chemical Neuroscience

T2 - ACS Chemical Neuroscience

JF - ACS Chemical Neuroscience

SN - 1948-7193

IS - 9

ER -