Talk:HDMP-28

Latest comment: 9 years ago by PharmaDharma in topic Discrimination ratio discrepancies

p,m-Cl2?

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What is the chemical listed on the table with a lower discrimination ratio than cocaine that's labled p,m-Cl2? 184.76.53.217 (talk) 04:09, 29 December 2010 (UTC)Reply

3,4-CTMP, though whether it's discrimination ratio adds to reinforcement as this article implies is contradicted in it's own article. Nagelfar (talk) 01:26, 6 August 2011 (UTC)Reply

Restricting methylnaphthidate's rotation for a new molecule.

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Restricted Rotation Analog (RRA) of Methylphenidate derivatives. Would a RRA of HDMP-28 cause any profile changes to DAT or SERT affinity? Nagelfar (talk) 01:23, 6 August 2011 (UTC)Reply

Discrimination ratio discrepancies

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The discrimination ratios specified in the table appear to be incorrect. In the Journal of Pharmacology and Therapeutics, D.R. values do not line up with those specified.

In the table, 3,4-CTMP (m,p-Cl2) is ranked above methylphenidate (Ph) (D.R. = 1.3, 2.7, respectively). In the Journal, threo-methylphenidate (TMP) is ranked above 3,4-CTMP (D.R. = 0.90  ± 0.09, 2.08  ± 0.05, respectively).

In the table, 4-methylmethylphenidate (p-Me) ranks more than a full point below threo-methylphenidate (Ph) (D.R. = 3.8, 2.7, respectively), while the Journal ranks these (4MeTMP, TMP) at near-parity (D.R. = 1.05  ± 0.02, 0.90  ± 0.09, respectively).

In the table, 3,4-CTMP (m,p-Cl2) ranks below cocaine by more than a full point (D.R.= 2.5, 1.3, respectively), while the Journal ranks these in the inverse, also by more than a full point ((−)-Cocaine, 3,4CTMP) (D.R. = 1.03  ± 0.01, 2.08  ± 0.05, respectively).

The cited sources do not contain any data outlining discrimination ratios for the β-Naphthyl. It appears as though this page's author calculated this on his or her own using [3H]DA figures as their sole guidepost. This is incorrect methodology, as all four compounds in question affect other monoamine transporters, all of which impact their discrimination ratios. Namely, cocaine and methylnaphthidate exhibit SERT blockade, while all four compounds blockade NET to varying degrees. It's for this reason that calculating discrimination ratios against DA uptake alone is imprecise. — Preceding unsigned comment added by PharmaDharma (talkcontribs) 02:55, 12 December 2014 (UTC)Reply