2016
DOI: 10.4172/2329-6631.1000162
|View full text |Cite
|
Sign up to set email alerts
|

Fentanyl - A Potent Opioid Analgesic: A Review

Abstract: We describe the computational design of proteins that bind the potent analgesic fentanyl. Our approach employs a fast docking algorithm to find shape complementary ligand placement in protein scaffolds, followed by design of the surrounding residues to optimize binding affinity. Co-crystal structures of the highest affinity binder reveal a highly preorganized binding site, and an overall architecture and ligand placement in close agreement with the design model. We use the designs to generate plant sensors for… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
3
1
1

Citation Types

0
11
0

Year Published

2021
2021
2024
2024

Publication Types

Select...
7

Relationship

0
7

Authors

Journals

citations
Cited by 9 publications
(11 citation statements)
references
References 39 publications
(25 reference statements)
0
11
0
Order By: Relevance
“…The thermal curve measured during TGA analysis of the fresh and degraded fentanyl is shown in Figure 4. For both powder types, a single mass-loss event was observed to begin at 232°C, which is the reported melting temperature for fentanyl HCl [15].…”
Section: Thermal Gravimetric Analysis/differential Scanning Calorimetrymentioning
confidence: 73%
“…The thermal curve measured during TGA analysis of the fresh and degraded fentanyl is shown in Figure 4. For both powder types, a single mass-loss event was observed to begin at 232°C, which is the reported melting temperature for fentanyl HCl [15].…”
Section: Thermal Gravimetric Analysis/differential Scanning Calorimetrymentioning
confidence: 73%
“…This morphinomimetic interacts mainly with presynaptic µ-opioid receptor of the central nervous system (review in Stanley, 2014 ). Its physicochemical characteristics allow it to cross the blood–encephalic barrier ( Terenius, 1974 ) and make it suitable for delivery by a transdermal therapeutic system ( Sharma et al, 2016 ).…”
Section: Discussionmentioning
confidence: 99%
“…Semi-synthetic and synthetic opioids used for treatment (e.g., codeine, hydrocodone, oxycodone, fentanyl and its analogs, tramadol, tapentadol, etc.) are very effective drugs for managing severe acute pain, cancer pain, and, in some cases, chronic non-tumor pain [ 2 , 3 , 4 ].…”
Section: Introductionmentioning
confidence: 99%
“…The risk is associated with dose-dependent respiratory depression, a common cause of death in the case of fatal intoxication [ 5 , 9 , 10 , 25 , 26 ]. The other symptoms of NSOs intoxication include, e.g., nausea, vomiting, constipation, sedation, cognitive impairment, and pruritus [ 3 ].…”
Section: Introductionmentioning
confidence: 99%