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  #1  
Old 21-10-2009, 04:47
956Vette 956Vette is offline
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The libido drug pt141

The Libido Drug
to find the link/source search men's journal magazine for libido, should be recent
Sept, 2009

The rise, fall, and stealth return of the world’s first medically proven aphrodisiac.
By Frederick Kaufman


As soon as the bremelanotide (a.k.a. PT-141) arrived in the mail, I shook the white crystal onto a mirror and began to chop it into powder. I snorted some and a bitter taste began its steady descent down the back of my throat. But I wasn’t about to complain. Thanks to a website called tanresearch dot com and $65, I finally had my hands on the most revolutionary sex drug ever created. This potion had undergone studies for almost a decade in a quest to make it the first-ever FDA-approved aphrodisiac to hit the U.S. market.

Sure, history and folk medicine are full of purported aphrodisiacs, like Spanish fly and rhinoceros horn. But bremelanotide isn’t like those — neither is it simply an erectile dysfunction drug like Viagra or Cialis, so-called PDE-5 inhibitors that work by pushing blood around the body. Bremelanotide belongs to a new class of drugs called melanocortins, which work in the mind, increasing sexual desire. Deep inside the brain, the substance stirs passion by activating hypothalamic and limbic emotional structures, the parts that naturally flare when you’re turned on. Scientists aren’t exactly sure how melanocortins do this, but the result is clear: Before you know it, you want to have sex. Or at least that’s what the research has shown.

After snorting 10 milligrams of the stuff, I felt nothing. Several hours later I still wasn’t the slightest bit horny. So at midnight I went to bed, totally unaware of the flood of animalistic desire that was to take hold of me.

A year earlier i was in the montreal lab of Jim Pfaus, arguably the world’s preeminent expert on bremelanotide.

A 50-year-old neuroscientist, Pfaus was in the last stages of preclinical trials aimed at getting FDA approval for bremelanotide. Originally developed as a self-tanning agent, the drug had been repurposed when male study subjects reported a surprising side effect: erections. A New Jersey pharmaceutical company called Palatin Technologies had bought the drug, then turned the pill into a powder that could be delivered nasally, hoping that sleek nasal-spray dispensers could blow away little blue pills — and earn profits that would dwarf the $150 million that Palatin had spent on research and clinical testing.

Pfaus showed me stunning testimonials from human test subjects. “On the five-point scale, I would rate the erection I had as a six,” said one of the 1,300 anonymous testers. “You get this humming feeling,” said another. “You’re ready to take your pants off and go.”

The drug worked equally well on women, who chronicled “an intense arousal” that lasted from six to 72 hours. “I was focused on sex,” said one of the women.

But there were side effects, and in 2007, Palatin’s sex drug hit a roadblock just before entering phase-three testing, the FDA’s final clinical hurdle before the drug is released to the public. Some of the men who sniffed bremelanotide experienced an increase in blood pressure, and about one third of the women who took the drug reported nausea.

There were also those who doubted the drug would actually cause couples to want to jump into bed together. “It’s baloney,” says Leonore Tiefer, a professor of psychiatry at New York University’s Langone School of Medicine. “You might increase genital itchiness, but you won’t increase desire.”

It appeared that bremelanotide would fall into the ash heap of failed aphrodisiacs, to rest in peace with tiger penis soup. But then something unexpected happened.

In 2008, Iranian urologist Mohammad Reza Safarinejad published findings he had gathered by testing bremelanotide that he purchased from a company in Dubai on men and women. “He got fantastic results,” says Pfaus. “Palatin had published everything about the drug — including the exact sequence of the compound.” Middle Eastern chemists used that sequence to create the drug themselves. Shortly thereafter, several companies began offering the drug online.

But was it safe? “Well,” says Pfaus, “we never resolved that blood pressure thing. There’s no guarantee of purity. The FDA won’t regulate it.”
  #2  
Old 23-10-2009, 01:53
956Vette 956Vette is offline
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Re: The libido drug pt141

Anyone able to post the link? Probably a better read...
  #3  
Old 06-01-2010, 18:16
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Re: The libido drug pt141

From Wikipedia

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 /brɛ ˌmɛ læ noʊ ˈtаɪd/ 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.

http://www.ncbi.nlm.nih.gov/pubmed/1...t=AbstractPlus

Palatin Technologies, Inc., Cranbury, New Jersey 08512, USA. ldiamond@palatin.com

OBJECTIVES: To evaluate the safety and pharmacodynamic effect of co-administration of subtherapeutic doses of PT-141, a cyclic heptapeptide melanocortin analogue, and sildenafil to patients with erectile dysfunction. METHODS: Nineteen patients with erectile dysfunction who were responders to either Viagra or Levitra by self-report were given 25 mg sildenafil and 7.5 mg intranasal PT-141, 25 mg sildenafil and an intranasal placebo spray, and a placebo tablet and an intranasal placebo spray in a randomized cross-over design. Erectile activity in response to two 30-minute episodes of visual sexual stimulation was assessed by RigiScan during a 6-hour postdose period. 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. 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. CONCLUSIONS: Co-administration of intranasal PT-141 and a phosphodiesterase type 5 inhibitor may constitute a treatment alternative for patients in whom higher doses of a single therapy are not effective or well tolerated.

PMID: 15833522 [PubMed - indexed for MEDLINE]

956Vette added 3 Minutes and 19 Seconds later...

What is Bremelanotide (PT-141)?

Bremelanotide (formerly PT-141) is the generic term for a new medication for use in treating sexual dysfunction in men (erectile dysfunction or impotence) as well as sexual dysfunction in women (sexual arousal disorder). It is a synthetic aphrodisiac. Unlike Viagra and other related medications, it does not act upon the vascular system, but directly increases sexual desire.

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 eight out of the ten original male volunteer test subjects. In clinical studies, bremelanotide has been shown to be effective in treating male sexual and erectile dysfunction as well as female sexual dysfunction. It is currently being tested by Palatin Technologies.

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). PT-141 is a metabolite of Melanotan II that lacks the C-terminal amide function. Its molecular formula is C50H68N14O10 with a molecular weight of 1025.2.
In the United States it is currently in a Phase III clinical trial.

Are these nasal? Oral, Injectable?

Currently the nasal and oral routes have not been made efficient. PT-141 is a sterile injectable made for sub-q injection, like insulin.

What's the dosing schedule...how much do I take?

.5mg-2mg is the range which people dose. Taking 2-4 hours before game time is ideal. The window of opportunity is very unique.

Say you had a dinner and movie arranged. Taking before dinner may be the best route, however during the climax of the movie may interfere with one of your own…read between the lines there

Is there any reconstituting involved?

Yes and bacteriostatic water is the recommended solvent here. To mix the vial with bact water, take one syringe (BD Ultrafine II 1cc or 1/3 cc are excellent and I recommend them) and grab your vial of bacteriostatic water. If using a 1 cc syringe (100 units), use the syringe to withdraw 1 full ml (1cc) and inject that into the vial of PT-141 through the rubber. Be sure to aim the needle towards the glass, so that it will trickle down and not harm the peptide. Swirl the vial to thoroughly mix and let the peptide dissolve. The key here is to be gentle. Say you had the vial of PT-141 stored in the freezer, move the vial of PT-141 to fridge for an overnight stay. Then you are ready the next day to reconstitute the same temperature refrigerated bact water with the PT-141 in the most efficient manner. Just some tricks of the trade here.

So now you have 100 units (1cc) of bacteriostatic water mixed with 10 mg of PT-141 in your vial ready to go. A 1mg dose would be 10 units or .1ml (.1cc). Make sense? Hope so.

How is it stored?

The lyophilized powder (freeze dried state) can be stored in the freezer or refrigerator. Once reconstituted (mixed with water) it will be good for a month in the refrigerator before it begins to degrade.

Does this help give erections or just put you in the mood?

“With PT-141, you feel good, not only sexually aroused,” reported anonymous patient 007, a participant in a Phase 2 trial, “you feel younger and more energetic.” Said another patient: “It helped the libido. So you have the urge and the desire. . . . You get this humming feeling; you’re ready to take your pants off and go.” And another: “Twice my wife and I had sex twice in one night. I came in [to work] and I just raved about it: ‘Jesus, guys . . . 58 years old and you don’t do that.’ ” Tales of pharmaceutically induced sexual prowess among 58-year-olds are common enough in the age of the Little Blue Pill, but they don’t typically involve quite so urgent a repertoire of humming, throbbing, tingling, and double-dipping. Or as patient 128 put it: “My wife knows. She can tell the difference between Viagra and PT-141.”

The precise mechanisms by which PT-141 does its job remain unclear, but the rough idea is this: Where Viagra acts on the circulatory system, helping blood flow into the penis, PT-141 goes straight to the brain itself. And there it goes to work, switching on the same neural circuitry that lights up when a person actually, you know, wants to.

Basically this takes men back to middle school. You may find yourself in a similar situation as you were in 8th grade science class with the teacher bent over helping the student in front of you. It may be necessary to do a “tuck up” if at the office…especially at the public pool!

Women state that the sensation given from injecting PT-141 is like being in heat! One colleague in particular stated that she didn’t know what was going on…but she had wanted “it” all day long after dosing the night before.

Last edited by 956Vette; 06-01-2010 at 18:16. Reason: Automerged Doublepost
  #4  
Old 06-01-2010, 22:12
markmorgan10 markmorgan10 is offline
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Re: The libido drug pt141

markmorgan10 added 6 Minutes and 9 Seconds later...

Speaking with SWIM, as someone who really doesn't want to inject - SWIM wants to know if there a great danger in just sniffing the powder ??

markmorgan10 added 0 Minutes and 15 Seconds later...

Speaking with SWIM, as someone who really doesn't want to inject - SWIM wants to know if there a great danger in just sniffing the powder ??

Last edited by Gradient; 02-12-2010 at 03:19. Reason: requesting sources
  #5  
Old 16-01-2010, 18:08
noiv noiv is offline
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Re: The libido drug pt141

Mrs. Swim gets good effects but also nausea which kills her desire
Does anyone know of an anti-nausea drug ?
  #6  
Old 04-03-2010, 19:10
956Vette 956Vette is offline
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Re: The libido drug pt141

Quote:
Originally Posted by noiv View Post
Mrs. Swim gets good effects but also nausea which kills her desire
Does anyone know of an anti-nausea drug ?
An anti-histamine (like Claritin) may be helpful
  #7  
Old 05-11-2012, 02:57
yrsofpainsucks yrsofpainsucks is offline
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Re: The libido drug pt141

So... Is it still avaliable or not? I was confused and the more I read it again the more confused I got
  #8  
Old 26-11-2012, 20:40
St Dismas Novitiate St Dismas Novitiate is offline
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Re: The libido drug pt141

Quote:
Originally Posted by noiv View Post
Mrs. Swim gets good effects but also nausea which kills her desire
Does anyone know of an anti-nausea drug ?
cannabis works well, as does ginger.

toxinreleased added 3 Minutes and 21 Seconds later...

I posted something on this when it first came out and have checked on it a few times since then. At last check, it was still not given final approval by the FDA for either its intended or its off the shelf uses. A quick google to check out the wiki should give updated information.

Last edited by St Dismas Novitiate; 26-11-2012 at 20:40. Reason: Automerged Doublepost

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