Talk:EXP-561

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I can't see the resemblance. The reference cited doesn't say anything about amphetamines. So what is going on here? —Preceding unsigned comment added by 87.108.64.117 (talk) 01:41, 31 August 2010 (UTC)[reply]

See this:

[1]

The resemblance of EXP-561 to amphetamine can be kind of hard to see due to the bicyclo[2.2.2]octane group. EXP-561 is basically amphetamine with the propyl chain replaced by the bicyclo[2.2.2]octane moiety; hence, a rigid analogue.

As for the reference:

"EXP-561 has some structural resemblance to amphetamine in having a phenyl group and a primary amine group separated about the same distance by aliphatic carbons."

Also:

"Rats are known to metabolize amphetamine primarily by hydroxylation of the para position of the phenyl ring. This metabolic route is blocked by iprindole and various other drugs; as a consequence, tissue levels of amphetamine are increased, its half-life is prolonged, and various pharmacologic effects of amphetamine are potentiated. We therefore determined if iprindole would affect tissue levels of EXP-561 and degree of uptake inhibition by EXP-561.....Iprindole pretreatment increased EXP-561 levels in brain and heart and prolonged its half-life, giving suggestive indirect evidence that EXP-561 may be metabolized in rats by ring hydroxylation in a manner similar to the metabolism of amphetamine."

el3ctr0nika (Talk | Contribs) 18:08, 31 August 2010 (UTC)[reply]

No, I just saw an overlay of amphetamine and this and the amines are 3.2Å apart. Amphetamine and this have no common structure whatsoever, just because they "may have similar metabolism" doesn't make them analogues.

Furthermore, amphetamine has 2 carbons between aryl & amine, this has 4 any way you look at it. — Preceding unsigned comment added by 87.108.64.117 (talk) 22:38, 2 September 2010 (UTC)[reply]

This article cites a lot of articles of no value, incorrectly compares with amphetamine & doesn't clearly state that this is an SDNRI drug, not a stimulant of any nature. — Preceding unsigned comment added by 86.30.243.179 (talk) 20:31, 18 September 2011 (UTC)[reply]

I would also add that in human studies, it was basically compared with tricyclics and a few one-off antidepressants (it proved ineffective treating depression) so even classing it as a stimulant is incorrect. It is basically an SNDRI and not a useful one at that. — Preceding unsigned comment added by 86.30.243.179 (talk) 10:53, 19 September 2011 (UTC)[reply]

It was a FAILED antidepressant as the references show. Perform a LogP function to see VERY slow onset. In fact, why aren't the SSRIs in stimulants? Are we listing stimulants, or drugs that have the side-effect of causing stimulation in some people?

I say move it or lose it.