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PT-141 (bremelanotide) is an experimental drug used for the purpose of sexual arousal. It is a melanocortin based peptide that has shown effectiveness in clinical studies on both male and female rats. Male rats have shown erectile response with doses as low as 1-2 mgs whereas most female rats have shown positive results with higher doses around 2-3 mgs. While the dosage requirements tend to be higher for female rats, the observable results in female rats tend to be stronger. An example of findings among male rats is displayed below in an abstract from this Palatin study:
PT-141, a cyclic heptapeptide melanocortin analog, was evaluated following intranasal administration in healthy male rats and in Viagra-responsive erectile dysfunction (ED) rats. Erectile response was assessed by RigiScan in healthy subjects without visual sexual stimulation (VSS) and in Viagra((R))-responsive ED patients with VSS. In healthy subjects, mean C(max) and AUC((0-t)) increased in a dose-dependent manner. Median T(max) was 0.50 h and mean t(1/2) ranged from 1.85 to 2.09 h. In both studies, an erectile response induced by PT-141 administration was statistically significant, compared to placebo, at doses greater than 7 mg, with the onset of the first erection occurring in approximately 30 min. PT-141 was safely administered and well tolerated in both studies. A maximum-tolerated dose was not identified. Flushing and nausea were the most common adverse events reported in both studies and no clinically significant changes in vital signs, laboratory tests, ECGs, or physical exams were observed.
Female rat responses can be seen here in this research abstract:
To review the effects of bremelanotide, an analogue of the naturally occurring peptide alpha-MSH, on the preclinical indices of sexual desire in female rats, and where in the brain these actions may occur. MAIN OUTCOME MEASURES: Appetitive sexual behaviors, such as solicitations, hops and darts, and pacing, were assessed along with consummatory behaviors such as lordosis. The involvement of brain regions was assessed following direct administration to the region, by the stimulation of molecular markers of neural activation, and using microdialysis to examine extracellular fluid for different neurotransmitters. METHODS: Using a model that allows ovariectomized, hormone-primed female rats to control the timing of sexual encounters with males, tested the ability of bremelanotide to increase appetitive (proceptive) and/or consummatory sexual behaviors. RESULTS: Bremelanotide dramatically and selectively increased measures of solicitation in female rats, without altering pacing or lordosis, following both peripheral (subcutaneous) administration or infusions directly into the lateral ventricles or medial preoptic area (mPOA), but not the ventromedial hypothalamus. The mPOA is critical for the display of appetitive sexual behaviors in females and males of a variety of species. Peripheral administration of bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior, and may work by activating dopamine terminals in the mPOA. CONCLUSIONS: To the extent that solicitations indicate the desire of female rats to engage in sexual activity, bremelanotide appears to possess the behavioral, pharmacological, and neuroanatomical specificity required of a drug in the treatment of hypoactive sexual desire disorders.
All research materials are USP grade materials. All materials sold on this site are sold for research purposes only.
Other great info on this product:
http://www.ncbi.nlm.nih.gov/pubmed/17958619?ordinalpos=5&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_DefaultReportPanel.Pubmed_RVDocSum
http://www.benthamdirect.org/pages/b_viewarticle.php
http://www3.interscience.wiley.com/journal/118592979/abstract
http://www3.interscience.wiley.com/journal/118592979/abstract
http://www.sciencebase.com/science-blog/libido-nasal-spray.html
http://nymag.com/lifestyle/sex/annual/2005/15061/
http://www.guardian.co.uk/science/2006/apr/23/medicineandhealth.observermagazine
References:
Diamond LE, Earle DC, Rosen RC, Willett MS, Molinoff PB. Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction, Int J Impot Res. 2004 Jan;16(1):51-9
Safarinejad MR., Evaluation of the safety and efficacy of bremelanotide, a melanocortin receptor agonist, in female subjects with arousal disorder: a double-blind placebo-controlled, fixed dose, randomized study., J Sex Med. 2008 Apr;5(4):887-97. Epub 2007 Dec 28.
PT-141, a cyclic heptapeptide melanocortin analog, was evaluated following intranasal administration in healthy male rats and in Viagra-responsive erectile dysfunction (ED) rats. Erectile response was assessed by RigiScan in healthy subjects without visual sexual stimulation (VSS) and in Viagra((R))-responsive ED patients with VSS. In healthy subjects, mean C(max) and AUC((0-t)) increased in a dose-dependent manner. Median T(max) was 0.50 h and mean t(1/2) ranged from 1.85 to 2.09 h. In both studies, an erectile response induced by PT-141 administration was statistically significant, compared to placebo, at doses greater than 7 mg, with the onset of the first erection occurring in approximately 30 min. PT-141 was safely administered and well tolerated in both studies. A maximum-tolerated dose was not identified. Flushing and nausea were the most common adverse events reported in both studies and no clinically significant changes in vital signs, laboratory tests, ECGs, or physical exams were observed.
Female rat responses can be seen here in this research abstract:
To review the effects of bremelanotide, an analogue of the naturally occurring peptide alpha-MSH, on the preclinical indices of sexual desire in female rats, and where in the brain these actions may occur. MAIN OUTCOME MEASURES: Appetitive sexual behaviors, such as solicitations, hops and darts, and pacing, were assessed along with consummatory behaviors such as lordosis. The involvement of brain regions was assessed following direct administration to the region, by the stimulation of molecular markers of neural activation, and using microdialysis to examine extracellular fluid for different neurotransmitters. METHODS: Using a model that allows ovariectomized, hormone-primed female rats to control the timing of sexual encounters with males, tested the ability of bremelanotide to increase appetitive (proceptive) and/or consummatory sexual behaviors. RESULTS: Bremelanotide dramatically and selectively increased measures of solicitation in female rats, without altering pacing or lordosis, following both peripheral (subcutaneous) administration or infusions directly into the lateral ventricles or medial preoptic area (mPOA), but not the ventromedial hypothalamus. The mPOA is critical for the display of appetitive sexual behaviors in females and males of a variety of species. Peripheral administration of bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior, and may work by activating dopamine terminals in the mPOA. CONCLUSIONS: To the extent that solicitations indicate the desire of female rats to engage in sexual activity, bremelanotide appears to possess the behavioral, pharmacological, and neuroanatomical specificity required of a drug in the treatment of hypoactive sexual desire disorders.
All research materials are USP grade materials. All materials sold on this site are sold for research purposes only.
Other great info on this product:
http://www.ncbi.nlm.nih.gov/pubmed/17958619?ordinalpos=5&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_DefaultReportPanel.Pubmed_RVDocSum
http://www.benthamdirect.org/pages/b_viewarticle.php
http://www3.interscience.wiley.com/journal/118592979/abstract
http://www3.interscience.wiley.com/journal/118592979/abstract
http://www.sciencebase.com/science-blog/libido-nasal-spray.html
http://nymag.com/lifestyle/sex/annual/2005/15061/
http://www.guardian.co.uk/science/2006/apr/23/medicineandhealth.observermagazine
References:
Diamond LE, Earle DC, Rosen RC, Willett MS, Molinoff PB. Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction, Int J Impot Res. 2004 Jan;16(1):51-9
Safarinejad MR., Evaluation of the safety and efficacy of bremelanotide, a melanocortin receptor agonist, in female subjects with arousal disorder: a double-blind placebo-controlled, fixed dose, randomized study., J Sex Med. 2008 Apr;5(4):887-97. Epub 2007 Dec 28.