A role for the melanocortin 4 receptor in sexual function
- Lex H. T. Van der Ploeg*,†,
- William J. Martin*,
- Andrew D. Howard*,
- Ravi P. Nargund*,
- Christopher P. Austin‡,
- Xiaoming Guan*,
- Jennifer Drisko*,
- Doreen Cashen*,
- Iyassu Sebhat*,
- Arthur A. Patchett*,
- David J. Figueroa*,
- Anthony G. DiLella*,
- Brett M. Connolly‡,
- David H. Weinberg*,
- Carina P. Tan*,
- Oksana C. Palyha*,
- Sheng-Shung Pong*,
- Tanya MacNeil*,
- Charles Rosenblum*,
- Aurawan Vongs*,
- Rui Tang*,
- Hong Yu*,
- Andreas W. Sailer*,
- Tung Ming Fong*,
- Cathy Huang*,
- Michael R. Tota*,
- Ray S. Chang‡,
- Ralph Stearns*,
- Constantin Tamvakopoulos*,
- George Christ§,
- Deborah L. Drazen¶,
- Brian D. Spar¶,
- Randy J. Nelson¶, and
- D. Euan MacIntyre*
- *Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065;‡ Merck Research Laboratories, West Point, PA 19486; §Albert Einstein College of Medicine, Montefiori Medical Center, Bronx, NY 10467; and¶ Department of Psychology and Neurosciences, Ohio State University, 09 Townshend Hall, Columbus, OH 43210
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Communicated by Charles R. Cantor, Sequenom, Inc., San Diego, CA (received for review December 27, 2001)
Abstract
By using a combination of genetic, pharmacological, and anatomical approaches, we show that the melanocortin 4 receptor (MC4R), implicated in the control of food intake and energy expenditure, also modulates erectile function and sexual behavior. Evidence supporting this notion is based on several findings: (i) a highly selective non-peptide MC4R agonist augments erectile activity initiated by electrical stimulation of the cavernous nerve in wild-type but not Mc4r-null mice; (ii) copulatory behavior is enhanced by administration of a selective MC4R agonist and is diminished in mice lacking Mc4r; (iii) reverse transcription (RT)-PCR and non-PCR based methods demonstrate MC4R expression in rat and human penis, and rat spinal cord, hypothalamus, brainstem, pelvic ganglion (major autonomic relay center to the penis), but not in rat primary corpus smooth muscle cavernosum cells; and (iv) in situ hybridization of glans tissue from the human and rat penis reveal MC4R expression in nerve fibers and mechanoreceptors in the glans of the penis. Collectively, these data implicate the MC4R in the modulation of penile erectile function and provide evidence that MC4R-mediated proerectile responses may be activated through neuronal circuitry in spinal cord erectile centers and somatosensory afferent nerve terminals of the penis. Our results provide a basis for the existence of MC4R-controlled neuronal pathways that control sexual function.
Footnotes
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↵ † To whom reprint requests should be addressed at: Department of Obesity and Metabolic Research, Merck Research Laboratories, 126 East Lincoln Avenue, Rahway, NJ 07076. E-mail: lex_van_der_ploeg{at}merck.com.
- Abbreviations:
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MC4R, melanocortin 4 receptor
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α-MSH, α-melanocyte stimulating hormone
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MCR, melanocortin receptor
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ICP, intracavernosal pressure
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ES cell, embryonic stem cell
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MAP, mean arterial pressure
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RT-PCR, reverse transcription–PCR
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CHO, Chinese hamster ovary
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THIQ, tetrahydroisoquinoline
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- Copyright © 2002, The National Academy of Sciences





