From Wiki Bremelanotide
Systematic (IUPAC) name
(3R,6R,9S,12R,15R,23R)-15-{[(2R)-2-
Acetamidohexanoyl]amino}-9-benzyl- 6-(3-carbamimidamidopropyl)-12- (1H-imidazol-5-ylmethyl)-3-(1H-indol- 3-ylmethyl)-2,5,8,11,14,17-hexaoxo- 1,4,7,10,13,18-hexaazacyclotricosane -23-carboxylic acid
Identifiers
CAS number 189691-06-3
ATC code ?
PubChem 23725087
Chemical data
Formula C50H68N14O10
Mol. mass 1025.2
SMILES eMolecules & PubChem
Bremelanotide (pronounced /br? ?m? læ no? ?t??d/ bremelanotide-pronunciation.ogg bremelanotide (help·info)) (formerly PT-141) is a compound under drug development by Palatin Technologies as a treatment for hemorrhagic shock and reperfusion injury. It functions by activating the melanocortin receptors MC1R and MC4R, to modulate inflammation and limiting ischemia. [1] It was originally developed for use in treating sexual dysfunction but this application was discontinued in 2008, after concerns were raised over adverse side effects of increased blood pressure.
Contents
[hide]
* * * 1 Development
* * * 2 Structure
* * * 3 See also
* * * 4 References
* * * 5 External links
Development
Originally, the peptide Melanotan II, that bremelanotide was developed from, was tested as a sunless tanning agent. In initial testing, Melanotan II did induce tanning but additionally caused sexual arousal and spontaneous erections as unexpected side effects in nine out of the ten original male volunteer test subjects.[2]
In studies, bremelanotide was shown to induce lordosis in an animal model [3] and be effective in treating sexual dysfunction in both men (erectile dysfunction or impotence) and women (sexual arousal disorder). Unlike Viagra and other related medications, it does not act upon the vascular system, but directly increases sexual desire via the nervous system. [4]
A Phase III clinical trial was scheduled to begin in the first half of 2007, but was delayed until August 2007. On August 30, Palatin announced that the U.S. Food and Drug Administration had expressed serious concerns regarding the risk/benefit ratio of bremelanotide with regards to the side effect of increased blood pressure. The FDA stated that they would consider alternate uses for bremelanotide, including as a treatment for individuals who do not respond to more established ED treatments. However, On May 13, 2008, Palatin Technologies announced it "has discontinued development of Bremelanotide for the treatment of male and female sexual dysfunction" however they concurrently announced plans to develop it as a treatment for hemorrhagic shock instead. [5] The company additionally announced intentions to focus its attention on another compound, PL-6983, that causes lower blood pressure in animal models. [6]
Structure
Bremelanotide is a cyclic hepta-peptide lactam analog of alpha-melanocyte-stimulating hormone (alpha-MSH) that activates the melanocortin receptors MC3-R and MC4-R in the central nervous system. It has the amino acid sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH or cyclo-[Nle4, Asp5, D-Phe7, Lys10]alpha-MSH-(4-10). It is a metabolite of Melanotan II that lacks the C-terminal amide function.
Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response.
[ncbi]
Palatin Technologies, Inc., Cranbury, New Jersey 08512, USA
OBJECTIVES]RESULTS: The erectile response induced by co-administration of PT-141 and sildenafil was significantly greater than the response elicited by administration of sildenafil alone.[/b] Co-administration of PT-141 and sildenafil was safe and well-tolerated and did not result in new adverse events or adverse events that were increased in frequency or severity compared with monotherapy. [b]CONCLUSIONS]
my experience with this product was great, using cialis with it was mind blowing and probably not something i will do again unless i was at a swing party that's for sure.. I can't remember the last time i was awakened 5 times during the night due to erections that would not go away..
"
my experience with this product was great, using cialis with it was mind blowing and probably not something i will do again unless i was at a swing party that's for sure.. I can't remember the last time i was awakened 5 times during the night due to erections that would not go away..
"
sunday (remember i administered on friday night)* I'm still amorous, the wife reports the same, more of a, "hey, you up for it again?? " kind of feeling
So it will be interesting to see how the effects continue to wain, or rather if they diminish over the next few days..
Due to no real knowledge of the correct ratio of melanotan 11 & the water to be mixed in the nasal apray bottle I have put two 10 m bottles of melanotan 11 with 30 ml of water.
Any input? too much? too little? and how many sprays?
"
Due to no real knowledge of the correct ratio of melanotan 11 & the water to be mixed in the nasal apray bottle I have put two 10 m bottles of melanotan 11 with 30 ml of water.
Any input? too much? too little? and how many sprays?
Thanks
"
Sorry to say you may have overdone things.* If I am understanding correctly...you have put 20mg MT-II into 30ml of water?*
How did you go about this sempainick?* Did you reconstitute both vials with 1ml of bact water for injection then extract into the bulk of the water?* Or did you remove the plastic flip top, aluminum, and rubber stopper in order to move the raw materials?
The peptide will degrade and may or may not be salvageable at this point.* Were you looking to get a tan or experience the aphrodisiac?
" Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response.
Pal Technologies, Inc., Cranbury, New Jersey 08512, USA.
OBJECTIVES]RESULTS: The erectile response induced by co-administration of PT-141 and sildenafil was significantly greater than the response elicited by administration of sildenafil alone.[/b] Co-administration of PT-141 and sildenafil was safe and well-tolerated and did not result in new adverse events or adverse events that were increased in frequency or severity compared with monotherapy. [b]CONCLUSIONS]
PMID]
"
I don't know about the nasal, but i did an injection of 2mg of the product subq.. then took 20mg of cialis, and i couldn't go to sleep, even after sex with the wife 3 times over the coarse of the evening..
Thank goodness she did the product with me, or i don't think she could have kept up..
Does it work?? wow.. yes, and you will be glad the next day if you can sneak a nap in..
Newbies here. Recently decided to try the PT141 from TR (subQ). First dose me - 0.5mg and the wife - 1mg. Brem flush and a few hours later mild sensations in the nether regions for both of us. Not really the WOW we were looking for. A week later we tried 1mg for me and 2mg for the wife. Pretty much the same results. Anybody have any comments on dosage or ideas about why neither of us are getting that 20 years younger feeling?* A newbie suggested dosage plan along with anticipated results would really be helpful at this point. Any constructive input will be greatly appreciated.
"
Newbies here. Recently decided to try the PT141 from TR (subQ). First dose me - 0.5mg and the wife - 1mg. Brem flush and a few hours later mild sensations in the nether regions for both of us. Not really the WOW we were looking for. A week later we tried 1mg for me and 2mg for the wife. Pretty much the same results. Anybody have any comments on dosage or ideas about why neither of us are getting that 20 years younger feeling?* A newbie suggested dosage plan along with anticipated results would really be helpful at this point. Any constructive input will be greatly appreciated.
"
Welcome lee.* Feel free to start a fresh thread to keep the focus and attn on you ]
Include some more info on a new topic with details such as to why you took 50% the dose of your other half...typically it is flipped.* Approx age, weight, stress, body mass, timing and expectations could be other valuable details.* Look forward to hearing more!
The stuff is certainly something that doesnt work for everyone, every time...but once understood and dialed in it can effectively give those youth feelings
"
my experience with this product was great, using cialis with it was mind blowing and probably not something i will do again unless i was at a swing party that's for sure.. I can't remember the last time i was awakened 5 times during the night due to erections that would not go away..
"
SacCat maybe there was overdose? i am not sure jus checkin
PT-141 Bremelanotide
The peptide structure of PT141 is almost identical to the endogenously produced melanocyte-stimulating hormone. PT141 is an agonist of the melanocortin-1 receptor which is located on melanocyte cells but it does not bind well to any other receptors.
Bremelanotide and or PT-141 have a much shorter amino acid sequence and a slightly different form than PT141. Because of this change binding to receptors other than the main melanocortin-1 receptor is much higher than that of Bremelanotide PT141. PT-141 also notably binds to two other receptors called receptor melanocortin-3 and receptor melanocortin-4.
PT-141 Bremelanotide Synthetic Melanocortin Aphrodisiac]Both PT-141 (Bremelanotide) and Melanotan II are analogs of the peptide hormone alpha melanocyte stimulating hormone. PT-141 and Bremelanotide have the amino acid sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH or cyclo-[Nle4, Asp5, D-Phe7, Lys10]alpha-MSH-(4-10) and a molecular weight of C50H68N14O10 1025.16 Dalton.
PT-141 Bremelanotide Physical Appearance]Filtered sterile white lyophilized powder in freeze dried form can appear broken up or in a solid cube which will dissolve upon impact of bacteriostatic sodium chloride for injection (or bac water/sterile water).
PT-141 Bremelanotide Reconstitution]It's recommended that you reconstitute the lyophilized PT141 or Bremelanotide in sterile bact water, which can then be further diluted to other water based solutions.
PT141 Bremelanotide Formulation]Protein (1mg/ml) was lyophilized with no additives.
PT141 Bremelanotide Stability]Lyophilized PT-141 & Bremelanotide although stable at room temperature for 3 weeks, should be stored in the fridge. After reconstitution MT-II should be stored also in the refrigerator days/weeks/months and for future use and experimentation at full potency.
Pharmaceutical Names of Actual and Related Peptides]Common Brand/Trade/Slang Names: Melanotan, Melanotan II, MT1, MTII, MT-II, MT2, MT-2
Amino Acid Molecule Chemical Structures]PT-141 - Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH or cyclo-[Nle4, Asp5, D-Phe7, Lys10]alpha-MSH-(4-10)
Molecular Formula and Molecular Weight]PT-141 -C50H68N14O10 1025.16 Dalton
Reply With Quote
