Delta Opiate Receptors

[Smyth]

Can anybody tell me anything about these?

 

[Sphinx (Afterlife)]

Delta receptors mediate spinal and supraspinal analgesia, dysphoria, psychotomimetic effects, as well - respiratory and vasomotor stimulation are caused by antagonist activity. Enkephalins are the endogenous ligand for these receptors.

Thats a start. Like most opioid receptors, most datas prolly gonna be conflicting.

 

[BilZ0r]

Looking for anything in particular?

 

[Smyth]

Just any gossip that you want to throw in.

http://www.ampainsoc.org/pub/bulletin/sep04/reso2.htm
http://www.scienceblog.com/community/older/2001/A/200110253.html

 

[Ivanhoe]

And can anyone tell me if Buprenorphine affects Delta receptors?

 

[BilZ0r]

Yes, looking at the PDSP, bupe has a Ki for delta around 1-20nM, for kappa 1-10nM, and Mu 0.5-10nM...

 

[C6H6]

Delta receptors mediate ... dysphoria, psychotomimetic effects...

Certainly not true. Delta agonists have very potent antidepressant effects and act as psychostimulants.

 

[BilZ0r]

^ Still, it's classical dogma, you'll find it in your Rang Dale and Ritter, and Goodman and Gillman for years to come.

 

[Sphinx (Afterlife)]

antidepressant effects through what mechanism of action? Direct Delta agonism??? Or is it like Mu agonism -> Gaba Inhibition -> Dopamine increase = mood enhancement?

 

[Sphinx (Afterlife)]

And would something that was a simultaneous Mu agonist and Delta Antagonist be capable of reducing respiratory depression from the Mu agonism?? If so, this would seem a logical pharmacokinetic attribute for 'less-taxing' opioids, yet retaining beleived euphoric Mu properties.

 

[BilZ0r]

I doubt the mood enchancing properties of opiates are due specifically, or even largely, to dopamine release.

 

[jacky]

in the mesolimbic systme there is a spot where the opiate and dopamine receptors are meshed. cross stimulation occurs in the release of dopamine. this may give rise to paradoxical stimulation. author/scientist James H Austin, in his book "zen and the brain" goes into depth about this .

 

[Smyth]

ya, this is exactly the type of feedback i was looking for when i posted this thread. so you think there is a place in the brain where opiate and dopamine are somehow 'related' to one another?

 

[BilZ0r]

Dopamine release may coincide with opiate release, but I strongly doubt there is much overlap in regards to functional consequences, like there is between dopamine and acetylcholine. *shrug* Maybe there is, but I doubt it.

 

[fastandbulbous]

cross stimulation occurs in the release of dopamine. this may give rise to paradoxical stimulation.

It's also dopamine release that can make using opiates a pukefest. Dopamine release in the CTZ generally means a bout of vomiting

 

[Limpet Chicken]

F&B, isn't that the reason apomorphine is so efficient as an emetic? because it is a direct dopamine agonist?

 

[BilZ0r]

^ Yup. Direct Dopamine D2, D3 agonists cause vomiting