World Library  
My Account |  Register |  Help  
  
Flag as Inappropriate
Email this Article

Methylnaphthidate

Article Id: WHEBN0024313773
Reproduction Date:

Title: Methylnaphthidate  
Author: World Heritage Encyclopedia
Language: English
Subject: Serotonin–norepinephrine–dopamine reuptake inhibitor
Collection:
Publisher: World Heritage Encyclopedia
Publication
Date:
 

Methylnaphthidate

HDMP-28 or methylnaphthidate is a piperidine based stimulant drug, closely related to methylphenidate, but with the phenyl ring replaced by naphthalene. It is a potent dopamine reuptake inhibitor, with several times the potency of methylphenidate and a short duration of action,[1] and is a structural isomer of another potent dopamine reuptake inhibitor, N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate.

Most of the TMP analogs of HDMP-28 have SERT Ki values in the range >10,000 and so are selective for dopamine and noradrenaline reuptake, with little or no effect on serotonin. HDMP-28 also has high affinity to SERT, and so behaves as a triple reuptake inhibitor.[2]

aEffect of (dl-threo) TMP and analogs on DA and 5HT Transporters.
Ar [3H]CFT DAT [3H]DA Uptake [3H]RTI-55 SERT Inhibition by 10μM D.R. Potency
Ph 83.9 224 >>10,000 19.6 2.7 1.00
p-F 35.0 142 >10,000 36.9 4.1 3.33
m-Cl 5.1 23.0 >10,000 45.5 4.5 2.42
p-Me 33.0 126 >10,000 45.0 3.8 0.74
p-NH2 34.5 114 >>10,000 7.9 3.3 2.18
m,p-Cl2 5.3 (2.67)b 7.0 1,064 (>10,000)b 93.3 1.3 7.98
β-Naphthyl 33.9b 11.0c 53.0c 71.6b nd 4.8c —
Cocaine 160 404 401 nd 2.5 0.41
aSchweri, et al. (2002);[3] bDavies, et al. (2004);[4] cDeutsch, et al. (2001).[5]

D.R. = Discrimination Ratio = [3H]DA ÷ [3H]CFT.

A low D.R. = addictive, whereas a high D.R. = low propensity for self-administration.

See also

References

This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and USA.gov, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for USA.gov and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
 
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
 
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.
 


Copyright © World Library Foundation. All rights reserved. eBooks from Project Gutenberg are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.