dc.contributor.author |
Jose, Jiney |
en |
dc.contributor.author |
Gamage, Swarnalatha |
en |
dc.contributor.author |
Harvey, MG |
en |
dc.contributor.author |
Voss, LJ |
en |
dc.contributor.author |
Sleigh, James |
en |
dc.contributor.author |
Denny, William |
en |
dc.coverage.spatial |
England |
en |
dc.date.accessioned |
2017-03-02T04:29:24Z |
en |
dc.date.available |
2013-06-19 |
en |
dc.date.issued |
2013-09-01 |
en |
dc.identifier.citation |
Bioorganic and Medicinal Chemistry, 01 September 2013, 21 (17), 5098 - 5106 |
en |
dc.identifier.issn |
0968-0896 |
en |
dc.identifier.uri |
http://hdl.handle.net/2292/32034 |
en |
dc.description.abstract |
A series of aliphatic esters of the non-opioid anaesthetic/analgesic ketamine were prepared and their properties as shorter-acting analogues of ketamine itself were explored in an infused rat model, measuring the time after infusion to recover from both the anaesthetic (righting reflex) and analgesic (response to stimulus) effects. The potency of the esters as sedatives was not significantly related to chain length, but Me, Et and i-Pr esters were the more dose potent (up to twofold less than ketamine), whereas n-Pr esters were less potent (from 2- to 6-fold less than ketamine). For the Me, Et and i-Pr esters recovery from anaesthesia was 10-15-fold faster than from ketamine itself, and for the n-Pr esters it was 20-25-fold faster than from ketamine. A new dimethylamino ketamine derivative (homoketamine) had ketamine-like sedative effects but was slightly less potent than, but ester analogues of homoketamine had very weak sedative effects. |
en |
dc.description.uri |
https://www.ncbi.nlm.nih.gov/pubmed/23876339 |
en |
dc.language |
English |
en |
dc.publisher |
Elsevier |
en |
dc.relation.ispartofseries |
Bioorganic and Medicinal Chemistry |
en |
dc.rights |
Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. Details obtained from http://www.sherpa.ac.uk/romeo/issn/0968-0896/
https://www.elsevier.com/about/company-information/policies/sharing |
en |
dc.rights.uri |
https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm |
en |
dc.subject |
Anaesthesia |
en |
dc.subject |
DCM |
en |
dc.subject |
Esters |
en |
dc.subject |
Ketamine |
en |
dc.subject |
LRR |
en |
dc.subject |
N-methyl-d-aspartate |
en |
dc.subject |
NMDA |
en |
dc.subject |
PWR |
en |
dc.subject |
Short-acting |
en |
dc.subject |
Structure–activity relationship |
en |
dc.subject |
dichloromethane |
en |
dc.subject |
loss of righting reflex |
en |
dc.subject |
pedal withdrawal reflex score |
en |
dc.subject |
Analgesics |
en |
dc.subject |
Animals |
en |
dc.subject |
Esters |
en |
dc.subject |
Female |
en |
dc.subject |
Heart Rate |
en |
dc.subject |
Ketamine |
en |
dc.subject |
Rats |
en |
dc.subject |
Rats, Sprague-Dawley |
en |
dc.subject |
Structure-Activity Relationship |
en |
dc.title |
Structure-activity relationships for ketamine esters as short-acting anaesthetics |
en |
dc.type |
Journal Article |
en |
dc.identifier.doi |
10.1016/j.bmc.2013.06.047 |
en |
pubs.issue |
17 |
en |
pubs.begin-page |
5098 |
en |
pubs.volume |
21 |
en |
dc.description.version |
VoR - Version of Record |
en |
dc.identifier.pmid |
23876339 |
en |
pubs.author-url |
http://www.sciencedirect.com/science/article/pii/S0968089613005786 |
en |
pubs.end-page |
5106 |
en |
pubs.publication-status |
Published |
en |
dc.rights.accessrights |
http://purl.org/eprint/accessRights/RestrictedAccess |
en |
pubs.subtype |
Article |
en |
pubs.elements-id |
405018 |
en |
pubs.org-id |
Medical and Health Sciences |
en |
pubs.org-id |
Medical Sciences |
en |
pubs.org-id |
Auckland Cancer Research |
en |
pubs.org-id |
School of Medicine |
en |
pubs.org-id |
Anaesthesiology |
en |
pubs.org-id |
Science |
en |
pubs.org-id |
Science Research |
en |
pubs.org-id |
Maurice Wilkins Centre (2010-2014) |
en |
dc.identifier.eissn |
1464-3391 |
en |
dc.identifier.pii |
S0968-0896(13)00578-6 |
en |
pubs.record-created-at-source-date |
2017-03-02 |
en |
pubs.online-publication-date |
2013-06-27 |
en |
pubs.dimensions-id |
23876339 |
en |