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Drug designs. (MedicinalUser SAR thread)

MedicinalUser247 said:
I call this one MD-Amino-Gamma-Plane. https://ibb.co/Pv6DhMjX
Click to expand...
^Structure reminds me of this molecule:

ALX 5407
N-[(3R)-3-([1,1'-Biphenyl]-4-yloxy)-3-(4-fluorophenyl)propyl]-N-methylglycine
[200006-08-2]

Layout does have a similarity to Prozac (fluoxetine) type structures, but with an additional acetic acid attached to the amine to give the glycine motif, i.e. Org 24598.

Selective non-transportable inhibitor of the glycine transporter GlyT1 (IC50 values are 3 nM and > 100 μM for human GlyT1c and GlyT2 respectively). Does not recognize other glycine sites, including the glycine site on the NMDA receptor (IC50 > 100 μM).

[1] Atkinson et al (2001) ALX 5407: a potent, selective inhibitor of the hGlyT1 glycine transporter. Mol.Pharmacol. 60 1414 PMID: 11723250
[2] Lipina et al (2005) Modulators of the glycine site on NMDA receptors, D-serine and ALX 5407, display similar beneficial effects to cloz. in mouse models of schizophrenia. Psychopharmacology 179 54 PMID: 15759151
 
[1] Brown, Angus; Carlyle, Ian; Clark, John; Hamilton, William; Gibson, Samuel; McGarry, George; McEachen, Sandra; Rae, Duncan; Thorn, Simon; Walker, Glenn (2001). "Discovery and SAR of Org 24598—A Selective Glycine Uptake Inhibitor". Bioorganic & Medicinal Chemistry Letters. 11 (15): 2007–2009. doi:10.1016/S0960-894X(01)00355-9.
[2] Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID: 23194655
 
MedicinalUser247 said:
Hi... I was just thinking about something. A lot of people say a Drug can only be Psychoactive if it contains a Nitrogen, but THC contains no Nitrogen at all. Yet THC is very Psychoactive. Would someone care to explain ?
Click to expand...

I Don't Know, But This One Might It Be A THC Agonist?

1-methyl-3-(2-hydroxy-4-pentylphenyl)piperidine.png


1-methyl-3-(2-hydroxy-4-pentylphenyl)piperidine
 
Regarding Your GHB Pharmacophore,
I Actually Prefer 1,4-BDO To GHB. Not That Doing Either Would Make My Life More Nearly Manageable Unless I Restricted My Impulse To Take More And More And More...
 
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