• N&PD Moderators: Skorpio | someguyontheinternet

Drug designs. (MedicinalUser SAR thread)

This agent is in the database but idk what it links to:
 
Just the amide of Tropacocaine works and is here in the database:
 
Yes, but I was trying to design something stronger.
Here let me show you this one:

3-(3,4-Dichloro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]oct-2-ene
PC10221020
Monoaminergic reuptake inhibitor S>N>D ordered TRI.
nM = 79 DA, 26 NE, 4.7 SER
Peter Moldt, Jørgen SCHEEL-KRÜGER, Gunnar M. Olsen, Elsebet Østergaard NIELSEN , WO1997013770 (1997 to Neurosearch A/S).

The N-demethylated compound is called HK3-263.

DAT 16nM, SERT 0.3nM, NET 20nM

Kaur H, Izenwasser S, Verma A, Wade D, Housman A, Stevens ED, Mobley DL, Trudell ML. Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6865-8. doi: 10.1016/j.bmcl.2009.10.087. Epub 2009 Oct 23. PMID: 19896846; PMCID: PMC2788963.

I suggest reading this patent as well: Dan Peters, Bjarne H. Dahl, John Paul Redrobe, Elsebet Østergaard NIELSEN, WO2007025978 (2007 to Neurosearch A/S).
 
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