trefentanil

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

trefentanil: RN refers to hydrochloride; a short-acting analgesic [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	60728
CHEMBL ID	84617
SCHEMBL ID	397177
MeSH ID	M0215069

Synonyms (19)

Synonym
trefentanyl
CHEMBL84617
a-3665 ,
trefentanil
n-[1-[2-(4-ethyl-5-oxotetrazol-1-yl)ethyl]-4-phenylpiperidin-4-yl]-n-(2-fluorophenyl)propanamide
L001379
unii-36qm58lvgu
120656-74-8
36qm58lvgu ,
trefentanil [inn]
trefentanil [who-dd]
n-(1-(2-(4-ethyl-4,5-dihydro-5-oxo-1h-tetrazol-1-yl)ethyl)-4-phenyl-4-piperidinyl)-n-(2-fluorophenyl)propanamide
trefentanil [mart.]
propanamide, n-(1-(2-(4-ethyl-4,5-dihydro-5-oxo-1h-tetrazol-1-yl)ethyl)-4-phenyl-4-piperidinyl)-n-(2-fluorophenyl)-
a-3665 free base
SCHEMBL397177
DTXSID80152955
DB09181
Q7837766

Research Excerpts

Dosage Studied

We determined the possible benefits of a new opioid, trefentanil, relative to fentanyl and alfent anil using high-resolution pharmacokinetic-pharmacodynamic modeling and computer simulations of clinical dosing scenarios. Finally, we used computer simulations to predict offset of opioid effects of trefenil, fentanyl, and alFENTanil when given in different dosing schemes.

Excerpt	Relevance	Reference
"We determined the possible benefits of a new opioid, trefentanil, relative to fentanyl and alfentanil using high-resolution pharmacokinetic-pharmacodynamic modeling and computer simulations of clinical dosing scenarios."	( Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Dyck, JB; Lemmens, HJ; Shafer, SL; Stanski, DR, 1994)	0.29
" Finally, we used computer simulations to predict offset of opioid effects of trefentanil, fentanyl, and alfentanil when given in different dosing schemes."	( Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Dyck, JB; Lemmens, HJ; Shafer, SL; Stanski, DR, 1994)	0.29
"We suggest that high-resolution pharmacokinetic-pharmacodynamic studies and computer simulations of clinical dosing scenarios may have significant usefulness in appreciating differences between new and established drugs in early phase I studies."	( Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Dyck, JB; Lemmens, HJ; Shafer, SL; Stanski, DR, 1994)	0.29

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

Assay ID	Title	Year	Journal	Article
AID114189	Analgesic activity in nonfasted male mice at 55 degree C using Hot plate assay	1989	Journal of medicinal chemistry, Dec, Volume: 32, Issue:12	4-Phenyl- and 4-heteroaryl-4-anilidopiperidines. A novel class of analgesic and anesthetic agents.
AID178398	Effective dose for its analgesic activity in male Sprague-Dawley rats using rat hot plate assay	1989	Journal of medicinal chemistry, Dec, Volume: 32, Issue:12	4-Phenyl- and 4-heteroaryl-4-anilidopiperidines. A novel class of analgesic and anesthetic agents.
AID189328	Analgesic activity was determined by observing the recovery of motor coordination in rats	1989	Journal of medicinal chemistry, Dec, Volume: 32, Issue:12	4-Phenyl- and 4-heteroaryl-4-anilidopiperidines. A novel class of analgesic and anesthetic agents.
AID178021	Effective dose for analgesic activity in male Sprague-Dawley rats using tail flick method	1989	Journal of medicinal chemistry, Dec, Volume: 32, Issue:12	4-Phenyl- and 4-heteroaryl-4-anilidopiperidines. A novel class of analgesic and anesthetic agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	1 (20.00)	18.7374
1990's	3 (60.00)	18.2507
2000's	1 (20.00)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	2 (40.00%)	5.53%
Reviews	1 (20.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	2 (40.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
histamine [no description available]	3.37	1	1	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
fentanyl Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.	6.07	3	1	anilide; monocarboxylic acid amide; piperidines	adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic
tramadol Tramadol: A narcotic analgesic proposed for severe pain. It may be habituating.. tramadol : A racemate consisting of equal amounts of (R,R)- and (S,S)-tramadol. A centrally acting synthetic opioid analgesic, used (as the hydrochloride salt) to treat moderately severe pain. The (R,R)-enantiomer exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. Originally developed by Gruenenthal GmbH and launched in 1977, it was subsequently isolated from the root bark of the South African tree Nauclea latifolia.. (R,R)-tramadol : A 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.	3.09	1	0	2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol	adrenergic uptake inhibitor; antitussive; capsaicin receptor antagonist; delta-opioid receptor agonist; kappa-opioid receptor agonist; metabolite; mu-opioid receptor agonist; muscarinic antagonist; nicotinic antagonist; NMDA receptor antagonist; opioid analgesic; serotonergic antagonist; serotonin uptake inhibitor
alfentanil Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position.	5.53	3	2	monocarboxylic acid amide; piperidines	central nervous system depressant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; peripheral nervous system drug
mirfentanil mirfentanil: selectively reverses the respiratory depressant effects of morphine; RN given refers to HCl; RN for parent cpd not available 9/91	3.09	1	0
remifentanil Remifentanil: A piperidine-propionate derivative and opioid analgesic structurally related to FENTANYL. It functions as a short-acting MU OPIOID RECEPTOR agonist, and is used as an analgesic during induction or maintenance of general anesthesia, following surgery, during childbirth, and in mechanically ventilated patients under intensive care.. remifentanil : A piperidinecarboxylate ester that is methyl piperidine-4-carboxylate in which the hydrogen attached to the nitrogen is substituted by a 3-methoxy-3-oxopropyl group and the hydrogen at position 4 is substituted the nitrogen of N-propanoylaniline.	3.09	1	0	alpha-amino acid ester; anilide; monocarboxylic acid amide; piperidinecarboxylate ester	intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; sedative
naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.	2.02	1	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
naloxonazine naloxonazine: binds irreversibly to opiate receptor sites; structure given in first source	7.02	1	0
piperidines Piperidines: A family of hexahydropyridines.	6.87	4	2

Condition	Relationship Strength	Studies	Trials
Ache [description not available]	3.37	1	1
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	3.37	1	1
Acute Post-operative Pain [description not available]	2.91	1	0
Pain, Postoperative Pain during the period after surgery.	2.91	1	0

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