Opiorphin

[Reminisant B]

Opiorphin

Any Ideas what this chemical looks like?

http://news.bbc.co.uk/1/hi/health/6142842.stm

The body's natural, non-euphoric morhpine by the sound of things.... In new scientist they mention it is a simple molecule and easy to synthesize.

?

 

[raybeez]

It's an endogenous peptide made up of 5 amino acids: Glutamine-Arginine-Phenylalanine-Serine-Arginine.

I'm somewhat confused as to how this compound works. It's administered to the rats IV and produces analgesia comparable to morphine.

The article says that "Opiorphin is the human functional homologue of the rat sialorphin, previously identified by a postgenomic approach as an inhibitor of pain perception that acts by potentiating mu- and delta- opiate receptor-dependent pathways".

So is the mechanism of analgesia simply potentiating endogenous opiate peptides, and not opiate receptor agonism?

--------------------------------

Abstract:

Wisner, A., et al. 2006. Proc Natl Acad Sci U S A. 13 Nov 06 [Epub ahead of print]. doi:10.1073/pnas.0605865103

Mammalian zinc ectopeptidases play important roles in turning off neural and hormonal peptide signals at the cell surface, notably those processing sensory information. We report here the discovery of a previously uncharacterized physiological inhibitor of enkephalin-inactivating zinc ectopeptidases in humans, which we have named Opiorphin. It is a QRFSR peptide that inhibits two enkephalin-catabolizing ectoenzymes, human neutral ecto-endopeptidase, hNEP (EC 3.4.24.11), and human ecto-aminopeptidase, hAP-N (EC 3.4.11.2). Opiorphin displays potent analgesic activity in chemical and mechanical pain models by activating endogenous opioid-dependent transmission. Its function is closely related to the rat sialorphin peptide, which is an inhibitor of pain perception and acts by potentiating endogenous micro- and delta-opioid receptor-dependent enkephalinergic pathways. Here we demonstrate the functional specificity in vivo of human Opiorphin. The pain-suppressive potency of Opiorphin is as effective as morphine in the behavioral rat model of acute mechanical pain, the pin-pain test. Thus, our discovery of Opiorphin is extremely exciting from a physiological point of view in the context of endogenous opioidergic pathways, notably in modulating mood-related states and pain sensation. Furthermore, because of its in vivo properties, Opiorphin may have therapeutic implications.

 

[IGNVS]

yeah i was wondering just that... there is hardly any information on it

 

[mad_scientist]

It's an endogenous peptide made up of 5 amino acids: Glutamine-Arginine-Phenylalanine-Serine-Arginine.

Wow thats a pretty simple peptide...would be pretty easy to make then, wonder how much one of those custom synth places that specialise in peptides would charge for it...also would be totally legal and seeing as its an endogenous compound in humans they might have trouble scheduling it...

 

[johanneschimpo]

^ good thinking

 

[MattPsy]

They scheduled DMT thou... heh
And GHB.

There are numerous other endogenous compound that are illegal too. We're all criminals !

 

[GABAlover]

Yawn, more spit-smoking dregheads.

 

[DopaMan]

Is this stuff able to pass the BBB when administered systemically? If so that would be neat. It would need its own transporter though...

 

[IGNVS]

Yawn, more spit-smoking dregheads.

hahaha...whats the concentration of this stuff... or here.. how bout the first person to tell me how much spit you would need to smoke (dry and wet weight) haha to get off on this stuff wins

 

[raybeez]

Is this stuff able to pass the BBB when administered systemically? If so that would be neat. It would need its own transporter though...

As far as I can tell from the article, it is able to pass the BBB. They give rats purified peptide via IV administration to their hind paws, and then demonstrate both analgesia and behavioral changes consistent with opiate intoxication. But I'm still unsure if the compound itself has any activity at opiate receptors, or if it instead acts by simply potentiating endogenous opiates.

 

[enoughorangejuice?]

sorry to reply to a year old thread but i was just reading about this (Opiorphin) on wikipedia and it says its relatively easy to produce in large quantities and is 6x as potent as morphine...just got me thinking

 

[Ham-milton]

DMT is a naturally occuring chemical, too, though. So is GHB.

I the peptide I want to try is brameletenoid (that's absolutely spelled wrong) the one that causes you to get horny.

 

[nuke]

Bremelanotide is what you're looking for.

 

[Limpet_Chicken]

Bremelanodide in DMSO anybody? strip club?

 

[kidamnesiac]

No, you need BenjaFranklamin in DMSO to get strippers horny.

 

[johanneschimpo]

^ its halloween night and i'm hammered but that made me laugh. then cough because I smoke too much

 

[rolls]

So no more news on this drug?

 

[mulberryman]

It's an endogenous peptide made up of 5 amino acids: Glutamine-Arginine-Phenylalanine-Serine-Arginine.

Wow thats a pretty simple peptide...would be pretty easy to make then, wonder how much one of those custom synth places that specialise in peptides would charge for it...also would be totally legal and seeing as its an endogenous compound in humans they might have trouble scheduling it...

God, I love the internet,,,

 

[5-HT2]

DMT is endogenous in humans, and they had no problem scheduling it

 

[qwe]

Morphine is also endogenous in humans
as is GHB

The body's natural, non-euphoric morhpine by the sound of things