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Effect of PDE-inhibitors on psychoactives?

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bigmac74

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Oct 13, 2005
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As far as i'm aware, phosphodiesterase inhibitors decrease the degradation of cAMP or cGMP. I know that cAMP is a secondary messenger used when norepinephrine binds to beta-adrenergic receptors, and I think that cAMP is a secondary messenger used by most other G-protein coupled receptors, so I was wondering, what effect would a PDE-inhibitor have on other drugs such as 5-HT2a agonists / releasers, opioids and GABA-agonists?

Also, at a high enough dose, would they have any psychoactive effects?
 
http://www.bluelight.ru/vb/showpost.php?p=2718305&postcount=45

cAMP is very important, but it is inhibited or stimulated, by GPCRs.

But yes, using PDE-inhibitors does stimulate B-adrenoreceptor like activity, i.e. why caffeine/theobromine makes your heart race and you lungs clear.

However, 5-HT2A is primarily Gq coupled, i.e. it is independent of cAMP.

Furthermore, it just doesn't work like that. Pertussin toxin (i.e. Whopping Cough) fucks Gi G-proteins, meaning an increase in cAMP. It just makes you very ill.

Simple pharmacology. More selective receptor targetting gives you the effects you want, without the ones you don't. i.e. Hit 1 receptors out of the 10,000 you have, and you get selective hallucinations. There are 3 major second messanger cascades, 1 out of 3 is not as selective as 1 out of 10,000.
 
BilZ0r said:
Simple pharmacology. More selective receptor targetting gives you the effects you want, without the ones you don't. i.e. Hit 1 receptors out of the 10,000 you have, and you get selective hallucinations. There are 3 major second messanger cascades, 1 out of 3 is not as selective as 1 out of 10,000.
Click to expand...

Okay, by the way, where did you find some of the information in that post, such as that 5-HT2a is a G-alpha-q subtype?

Also, say I were to take a drug that inhibited the enzyme that destroyed IP3 / DAG, at the same time as taking a 5-HT2a agonist, would it amplify the effect? (along with some side effects of course).
 
^^^who the fuck knows. It is unclear which intracellular signaling pathways mediate the hallucinogenic effects of certain agonists.
 
lf hsa;lnfsdklnf ekn;vd nsg hvhi opkjbvw rngvwojhs nlm; vboisd vnls vjospadv w ,SC HVOPSD NWInsal; ana nvsjanijnwrj ,. j nsdsjnvsd,m/.asj.
 
Helios. said:
lf hsa;lnfsdklnf ekn;vd nsg hvhi opkjbvw rngvwojhs nlm; vboisd vnls vjospadv w ,SC HVOPSD NWInsal; ana nvsjanijnwrj ,. j nsdsjnvsd,m/.asj.
Click to expand...

wtf?
 
BilZ0r said:
Where did I get 5-HT2A is primarily Gq, 7 years of pharmacology education... Pharmacology by Rang Dale and Ritter, that IUPHAR review on serotonin receptors in by Hoyer in Pharmacology Reviews... uh:
http://www.ncbi.nlm.nih.gov/entrez/...t_uids=7938165&query_hl=3&itool=pubmed_docsum

Yeah.
Click to expand...

Okay thanks, I also saw it on the 5-HT receptor wikipage (after you posted though).

The only problem is, wikipedia doesn't always have the answers, I thought there might be a site with all the known "which receptor uses which secondary messenger".
 
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