10 replies to this topic

[bernard]

As you guys probably know there is a peptide called Bremelanotide formerly known as PT-141. To make a long story short, there is this other peptide called Melanotan II which was used to induce Sunless and UVless tanning and people found out that it results in a very strong libido boost both in men and women as well. The reason for that was the fraction now known as Bremelanotide. Bremelanotide is an isolated fraction that is used for the purpose of treating sexual dysfunction. Now I'm not talking about the effect one would get from Viagra or Cialis. I'm talking directly affecting the brain to increase sexual desire. This happens by stimulating the MC1R, MC3R and MC4R melanocortin receptors.

I've tried this peptide and let me tell you this - It works like magic. Just 4 hours after a subQ injection and even the slightest hint of skin will awaken the rabbit inside you. That goes on for 1-3 days. As you will read in the wiki article - at first it was developed to be introduced through a nasal spray which however resulted in very high peak plasma levels and high blood pressure. So they switched to subQ injections and voila, no more blood pressure side effects due to a much slower introduction to the blood stream.

Now while this is a cool tool to have peptides are not very comfortable. First of all you need to keep them in a separate sterile fridge. Second of all you need to reconstitute with acetic acid and bacteriostatic water every now and then and last but not least some people are not comfortable with injections. I don't mind but a lot of people do. So here is what I was thinking. If we take the knowledge from this peptide maybe we could find a way out to activate the MC1R, MC3R and MC4R receptors through dietary or supplemental intake. What if there are foods/herbs/amino acids (after all peptides are fractions of amino acids) that can stimulate these receptors in a more subtle and long-term way. This can fix every couple's love life forever. Not only this but studies show that activating melanocortin receptors might greatly reduce inflammation which can be useful in a lot of people:

Check this out:
1. Natural and synthetic agonists of the melanocortin receptor type 3 possess anti-inflammatory properties
2. Targeting Melanocortin Receptors as a Novel Strategy to Control Inflammation

According to Wiki:
"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."

Knowing this, could we come up with ways to activate these receptors through dietary intake ? Can't wait to see what you think about this.

[gizmobrain]

I would guess at least one of the many herbs that are targeted towards sexual desire would have an affinity for these receptors. Obviously some are just dopamine boosters, some are PDE5 inhibitors, but at least one probably works on this same mechanism.

From there, it would be isolating which compound is responsible, and then finding a method of extraction (and hoping that someone else has already done the ground work for you, unless you are wanting to market it yourself).

I know this is vague, but I just thought I'd throw it out there.

[bernard]

I'm not actually looking to profit out of this. It's just for personal benefits. In fact I'd be a regular customer to anyone who finds out the formula.

I think PDE5 inhibitors don't really work for sexual drive just for erectile dysfunction, but maybe I'm wrong.

Edited by Tatsumaru, 13 August 2012 - 06:53 PM.

[gizmobrain]

I think PDE5 inhibitors don't really work for sexual drive just for erectile dysfunction, but maybe I'm wrong.

Yep, that's what I meant by "some are just PDE5 inhibitors" like Epimedium (horny goat weed), meaning they only increase blood flow.

Sexual desire is a whole other realm, like you seem to already know. Some herbs are taken to increase desire, so these are the ones I would start with researching their supposed mechanisms. I think Catuaba is mostly a dopamine increaser, but start by researching the mechanisms of Muira Puama, Tribulus, and Maca. These are pretty common. I'm sure with the hundreds of entheogen, ayurvedic, or asian herbs that are supposed to increase sexual desire, at least one must work on melanocortin receptors, right?

[gizmobrain]

For instance, Hoodia:

' class='bbc_url' title='External link' rel='nofollow external'>http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2700180']
Figure 1
Trirhabinoside, 14-OH, 12-tigloyl pregnane steroidal glycoside named P57A53A53 isolated from Hoodia (Van Heerden et al., 2007).

3.3.3 Mechanism(s) of action

P57A53 may simultaneously act on multiple body systems. Hypotheses include impeding gastric secretions (Hakkinen et al., 2004) or gastric emptying (Van Heerden et al., 2007), which are likely actions on the peripheral nervous system, and different mechanisms of CNS activity affecting energy homeostasis sensing in the hypothalamus. ICV injection directly into rat brains reduces appetite, demonstrating a direct CNS mechanism (MacLean & Luo, 2004). It has been suggested that this action involves the melanocortin-4 receptor, regulating neuropeptide “Y” (which is negatively regulated by leptin) and increasing cholecystokinin, which inhibits gastric emptying (Van Heerden et al., 2007). Hypothalamic ATP content is altered by ICV injection of P57A53, elevating ATP in the hypothalami of rats fed a normal diet, and impeding the otherwise witnessed decrease in ATP in the hypothalami of underfed rats. It increases the concentration of K⁺ in cells by acting as a non-binding antagonist to g-straphanthin/ouabain’s effect of decreasing intracellular K⁺ concentrations (shown by ⁸⁶RB proxy) through its action on Na⁺, K⁺-ATPase (the Na⁺ pump). The specific mechanism of this action is not yet clear; although P57A53 does not bind to Na⁺, K⁺-ATPase as the cardenolides do, it is hypothesized to affect another ATP-ase regulating K⁺ channels. P57A53 can clearly serve as a useful probe for further investigation into mechanisms of CNS energy sensing, which could lead to treatment of energy homeostasis disorders that can cause obesity and insulin resistance (Levin & Routh, 1996; MacLean & Luo, 2004).

→ source (external link)

Edited by zrbarnes, 13 August 2012 - 07:22 PM.

[gizmobrain]

Looking through anecdotes of genuine (not the cheapo supplements found in every supermarket) Hoodia side-effects, it would appear increased libido is common, so this is not a long shot.

[bernard]

Isn't inhibition of gastric emptying something one would want to avoid though ?

He Shou Wu is something I take which is a powerful aphrodisiac. Maybe it has something to do with it.

[gizmobrain]

Isn't inhibition of gastric emptying something one would want to avoid though ?

He Shou Wu is something I take which is a powerful aphrodisiac. Maybe it has something to do with it.

Most of the research on melanocortin receptors has to do with weight loss and obesity. There is a lot of psychoactive substances that cause changes in our bodies as an indirect result. It's just the nature of the beast.

You really have to look at the real world implication of it. To that, I have no knowledge. It may be beneficial or detrimental. I was just throwing it out there as one of the few plants on Pubmed that have possible effects on melanocortin receptors.

Usually, for these kinds of things to work, you need a stack of a few things that enhance the effects you are looking for, and minimize those you don't.

[chris106]

Well, looks like a compund that works with that mechanism is now available at TLR...

http://teamtlr.com/s...html#/amount-1g

[Area-1255]

 

Isn't inhibition of gastric emptying something one would want to avoid though ?

He Shou Wu is something I take which is a powerful aphrodisiac. Maybe it has something to do with it.

Most of the research on melanocortin receptors has to do with weight loss and obesity. There is a lot of psychoactive substances that cause changes in our bodies as an indirect result. It's just the nature of the beast.

You really have to look at the real world implication of it. To that, I have no knowledge. It may be beneficial or detrimental. I was just throwing it out there as one of the few plants on Pubmed that have possible effects on melanocortin receptors.

Usually, for these kinds of things to work, you need a stack of a few things that enhance the effects you are looking for, and minimize those you don't.

 

There's a lot of complex interactions here, but to assume that melanocortins are automatically involved in a MOA of a particular product because of effects on  libido, weight loss or any other specific parameter, is quite narrow IMHO.

There are MANY things that interact with and tune in to the hypothalamus - and also many things that influence a-MSH (alpha melanocyte stimulating hormone) - with this mindset though - you might as well say Copper is an aphrodisiac because it raises melanin and can suppress appetite due to being a stimulant. Yet nothing is further from the truth, copper opposes zinc and histamine - both of which yield negative effects upon libido.

 

Yet the irony yet again, copper lowers histamine levels and yet raises melanin, but yet histamine also raises melanin/a-MSH etc

Copper stimulates the hypothalamus at low amounts, whereas high amounts it decreases the general activity of hypothalamic neurons.

 

Histamine stimulates pigmentation and Melanocytes

                                                                        http://www.ncbi.nlm....pubmed/11071848  (Inverse Regulation)

 

                                                                            A-MSH stimulates Histamine?

 

http://www.livestron...create-melanin/

 

http://www.ncbi.nlm..../pubmed/1600517

 

http://www.ncbi.nlm....les/PMC1345683/

 

 

Edited by Area-1255, 17 September 2014 - 11:21 PM.

[Flex]

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