Flutamide and cyproterone acetate exert agonist effects: induction of androgen receptor-dependent neuroprotection. 2007

Thuy-Vi V Nguyen, and Mingzhong Yao, and Christian J Pike
University of Southern California, Davis School of Gerontology, 3715 McClintock Avenue, Los Angeles, CA 90089-0191, USA.

Androgens can exert profound effects on the organization, development, and function of the nervous system through activation of androgen receptors (ARs). Nonsteroidal and steroidal antiandrogens antagonize AR-mediated, classic genomic actions of androgens. However, emerging studies in nonneuronal cells indicate that antiandrogens can act as partial agonists for the AR. Here we investigated the effects of the antiandrogens flutamide and cyproterone acetate on neuroprotection induced by dihydrotestosterone (DHT). We observed that, although flutamide and cyproterone acetate blocked androgen-induced gene expression, they failed to inhibit DHT protection against apoptotic insults in cultured hippocampal neurons. Interestingly, flutamide and cyproterone acetate alone, like DHT, significantly reduced apoptosis. Furthermore, the protective actions of flutamide and cyproterone acetate were observed specifically in AR-expressing cell lines, suggesting a role for AR in the agonist effects of antiandrogens. Our results indicate that, in contrast to the classic antiandrogen properties of flutamide and cyproterone acetate, these AR modulators display agonist activities at the level of neuroprotection. These findings provide new insight into the agonist vs. antagonist properties of antiandrogens, information that will be crucial to understanding the neural implications of clinically used AR-modulating drugs.

UI MeSH Term Description Entries
D009474 Neurons The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM. Nerve Cells,Cell, Nerve,Cells, Nerve,Nerve Cell,Neuron
D011944 Receptors, Androgen Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA. Androgen Receptors,5 alpha-Dihydrotestosterone Receptor,Androgen Receptor,Dihydrotestosterone Receptors,Receptor, Testosterone,Receptors, Androgens,Receptors, Dihydrotestosterone,Receptors, Stanolone,Stanolone Receptor,Testosterone Receptor,5 alpha Dihydrotestosterone Receptor,Androgens Receptors,Receptor, 5 alpha-Dihydrotestosterone,Receptor, Androgen,Receptor, Stanolone,Stanolone Receptors,alpha-Dihydrotestosterone Receptor, 5
D005485 Flutamide An antiandrogen with about the same potency as cyproterone in rodent and canine species. Niftolid,Apimid,Apo-Flutamide,Chimax,Cytamid,Drogenil,Euflex,Eulexin,Eulexine,Fluken,Flulem,Flumid,Fluta 1A Pharma,Fluta-GRY,Fluta-cell,Flutamin,Flutandrona,Flutaplex,Flutexin,Fugerel,Grisetin,Niftolide,Novo-Flutamide,Oncosal,PMS-Flutamide,Prostacur,Prostica,Prostogenat,SCH-13521,Testotard,Apo Flutamide,ApoFlutamide,Fluta GRY,Fluta cell,FlutaGRY,Flutacell,Novo Flutamide,NovoFlutamide,PMS Flutamide,SCH 13521,SCH13521
D005786 Gene Expression Regulation Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation. Gene Action Regulation,Regulation of Gene Expression,Expression Regulation, Gene,Regulation, Gene Action,Regulation, Gene Expression
D000726 Androgen Antagonists Compounds which inhibit or antagonize the biosynthesis or actions of androgens. Androgen Antagonist,Antiandrogen,Antiandrogens,Anti-Androgen Effect,Anti-Androgen Effects,Antiandrogen Effect,Antiandrogen Effects,Antagonist, Androgen,Antagonists, Androgen,Anti Androgen Effect,Anti Androgen Effects,Effect, Anti-Androgen,Effect, Antiandrogen,Effects, Anti-Androgen,Effects, Antiandrogen
D000728 Androgens Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power. Androgen,Androgen Receptor Agonist,Androgen Effect,Androgen Effects,Androgen Receptor Agonists,Androgenic Agents,Androgenic Compounds,Agents, Androgenic,Agonist, Androgen Receptor,Agonists, Androgen Receptor,Compounds, Androgenic,Effect, Androgen,Effects, Androgen,Receptor Agonist, Androgen,Receptor Agonists, Androgen
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000831 Animals, Newborn Refers to animals in the period of time just after birth. Animals, Neonatal,Animal, Neonatal,Animal, Newborn,Neonatal Animal,Neonatal Animals,Newborn Animal,Newborn Animals
D016716 PC12 Cells A CELL LINE derived from a PHEOCHROMOCYTOMA of the rat ADRENAL MEDULLA. PC12 cells stop dividing and undergo terminal differentiation when treated with NERVE GROWTH FACTOR, making the line a useful model system for NERVE CELL differentiation. Pheochromocytoma Cell Line,Cell Line, Pheochromocytoma,Cell Lines, Pheochromocytoma,PC12 Cell,Pheochromocytoma Cell Lines
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats

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