A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects

A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects

Prescription opioids, such as morphine, remain an important part in the management of pain. However, their clinical utility can be limited by side effects such as constipation, nausea, and high risk of addiction. Additionally, abuse of prescription opioids has been on the rise in recent years. There...

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Main Author: Brookshire, Stephen William
Language:en
Published: The University of Arizona. 2012
Online Access:http://hdl.handle.net/10150/243897
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spelling ndltd-arizona.edu-oai-arizona.openrepository.com-10150-2438972015-10-23T04:57:04Z A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects Brookshire, Stephen William Prescription opioids, such as morphine, remain an important part in the management of pain. However, their clinical utility can be limited by side effects such as constipation, nausea, and high risk of addiction. Additionally, abuse of prescription opioids has been on the rise in recent years. Therefore, it is necessary to develop effective analgesics that lack the rewarding properties of currently used opioids. The neurokinin-1 receptor (NK-1) and its endogenous ligand, Substance P (SP), have been implicated in the control of nausea and vomiting, as well as mediating the rewarding effects of opioids. Here we have characterized the side effects of a novel efficacious opioid agonist/NK-1 antagonist, TY027. TY027 fails to elicit conditioned place preference, retching or vomiting, and does not inhibit gastric motility. These findings suggest that TY027 has a superior side effect profile when compared to currently used opioids, and most importantly, it does not produce rewarding effects that may lead to addiction. 2012-05 text Electronic Thesis http://hdl.handle.net/10150/243897 en Copyright © is held by the author. Digital access to this material is made possible by the University Libraries, University of Arizona. Further transmission, reproduction or presentation (such as public display or performance) of protected items is prohibited except with permission of the author. The University of Arizona.
collection NDLTD
language en
sources NDLTD
description Prescription opioids, such as morphine, remain an important part in the management of pain. However, their clinical utility can be limited by side effects such as constipation, nausea, and high risk of addiction. Additionally, abuse of prescription opioids has been on the rise in recent years. Therefore, it is necessary to develop effective analgesics that lack the rewarding properties of currently used opioids. The neurokinin-1 receptor (NK-1) and its endogenous ligand, Substance P (SP), have been implicated in the control of nausea and vomiting, as well as mediating the rewarding effects of opioids. Here we have characterized the side effects of a novel efficacious opioid agonist/NK-1 antagonist, TY027. TY027 fails to elicit conditioned place preference, retching or vomiting, and does not inhibit gastric motility. These findings suggest that TY027 has a superior side effect profile when compared to currently used opioids, and most importantly, it does not produce rewarding effects that may lead to addiction.
author Brookshire, Stephen William
spellingShingle Brookshire, Stephen William
A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects
author_facet Brookshire, Stephen William
author_sort Brookshire, Stephen William
title A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects
title_short A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects
title_full A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects
title_fullStr A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects
title_full_unstemmed A Novel Bifunctional Opioid That Lacks Traditional Opioid Side Effects
title_sort novel bifunctional opioid that lacks traditional opioid side effects
publisher The University of Arizona.
publishDate 2012
url http://hdl.handle.net/10150/243897
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AT brookshirestephenwilliam novelbifunctionalopioidthatlackstraditionalopioidsideeffects
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