Bw373u86

[lolwhatzdrugs]

BW373U86, anyone heard of it?

molecular structure

NSFW:

Claims about it on wikipedia sound odd

"although the convulsive effect is reduced when it is co-administered with μ-opioid agonists.[10] Another advantage of the combination is that BW373U86 reverses the respiratory depression produced by μ-opioid agonists, without affecting pain relief.[11]"

 

[Seppi]

That was a random fact from a study on rats (every study on that page at the moment is based upon rats). Shouldn't have been included in that article without specifying that. I cut it because that's not necessarily relevant or true for humans.

Thanks for pointing that out though.

 

[Hammilton]

Delta agonist, right?

 

[lolwhatzdrugs]

Delta agonist, right?

δ agonist 15x the strength of μ agonism. According to wiki, sourced with

Abstract
Four different opioid receptor binding assays and three different isolated tissue studies were used to screen for delta receptor-selective nonpeptidic compounds. (+/-)-4-((alpha-R*)-alpha-((2S*,5R*)-4-Allyl-2,5- dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N,N-diethylbenzamide (BW373U86) was a potent delta receptor-selective ligand in receptor binding assays. The Ki values were 1.8 +/- 0.4, 15 +/- 3, 85 +/- 4 and 34 +/- 3 nM for delta, mu, epsilon and kappa receptor binding sites, respectively. BW373U86 inhibited electrically evoked muscle contraction of mouse vas deferens with an ED50 value of 0.2 +/- 0.06 nM. This inhibitory effect of BW373U86 was antagonized by the delta receptor-selective antagonist naltrindole in a competitive manner: the Schild plot indicated a slope of 1 and a pA2 value of 9.43 (Ke = 3.7 x 10(-10) M), which is consistent with the high affinity of naltrindole in delta receptors. BW373U86 did not interact significantly with other receptors. BW373U86 inhibited the acoustic startle reflex after subcutaneous administration from 0.2- to 2-mg/kg doses in rats, and this inhibition was blocked by naltrindole. BW373U86 also induced a dose-dependent increase of locomotor activity in rats at similar doses. This effect was inhibited by naltrindole. These data suggest that BW373U86 is a potent and selective nonpeptidic delta agonist, and it elicits distinct in vivo pharmacological activities.
PMID: 8246159 [PubMed - indexed for MEDLINE]

https://www.ncbi.nlm.nih.gov/pubmed/8246159

 

[Lightning-Nl]

Almost looks like a derivative of Hydroxyzine lol. Maybe even a cyclic derivative of pethidine. Of course, that's just what it LOOKS like. Not saying it is...

Anyways, I've noticed an odd relationship between NMDA antagonists, Muscarinic antagonists, and μ-opioid agonists. Seems like many derivatives of those three classes are intertwined in terms of receptor affinity. Perhaps the structure of the NMDA, Muscarinic, and μ-opioid receptors are similar?

 

[lolwhatzdrugs]

Like methadone (without being an muscarinic antagonists)?

 

[Lightning-Nl]

Like methadone (without being an muscarinic antagonists)?

Yup, other good examples are Diphenidine, Diphenhydramine, Tramadol, Pethidine, Methorphan (Dextro & Levo), Ketamine, Methoxetamine... the list goes on...

 

[ebola?]

Anyways, I've noticed an odd relationship between NMDA antagonists, Muscarinic antagonists, and μ-opioid agonists. Seems like many derivatives of those three classes are intertwined in terms of receptor affinity

The SAR space for nmda-antagonism is really wide.

ebola