Compounds > thienorphine
Page last updated: 2024-10-15

thienorphine

Description

thienorphine: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID154735175
MeSH IDM0500708

Synonyms (2)

Synonym
thienorphine
DTXSID401018242

Research Excerpts

Overview

Thienorphine hydrochloride is a new anti-relapse drug for opioid abusers. It is currently under a Phase II clinical trial in China as a new treatment for opioid dependence.

ExcerptReference
"Thienorphine hydrochloride is a new anti-relapse drug for opioid abusers that is currently in phase II clinical trial. "( Thienorphine induces antinociception without dependence through activation of κ- and δ-, and partial activation of μ- opioid receptor.
Chen, M; Gong, Z; Li, Y; Su, R; Yong, Z; Zhang, Y; Zhou, P, 2020)
"Thienorphine is a new, non-selective partial agonist of opioid receptors. "( Up-regulation of monoamine oxidase activity in the striatum of rats following chronic treatment of thienorphine.
Gong, Z; Su, R; Wang, X; Yan, L; Yong, Z, 2013)
"Thienorphine is a new nonselective partial agonist of opioid receptors, which is currently under a Phase II clinical trial in China as a new treatment for opioid dependence. "( The effect of chronic thienorphine administration on long-term potentiation and synaptic structure in rat hippocampus.
Dong, Z; Gong, Z; Su, R; Wang, X; Yan, L; Yong, Z, 2013)
"Thienorphine is a partial opioid agonist that is a good candidate for the treatment of opioid dependence; however, to date, no studies have reported the effects of thienorphine on the function of the biliary tract."( Effects of thienorphine on contraction of the guinea pig sphincter of Oddi, choledochus and gall bladder.
Gong, Z; Li, T; Su, R; Zhou, P, 2014)
"Thienorphine is a partial opioid agonist that is a good candidate for the treatment of opioid dependence and pain."( Effects of thienorphine on the contraction of isolated ureter and bladder of guinea pigs.
Gong, Z; Li, Y; Su, R; Yan, H; Yong, Z; Zhou, P, 2016)
"Thienorphine is a chemically-new opioid developed in Beijing Institute of Pharmacology and Toxicology. "( [Structure-activity relationships analysis of thienorphine and its derivatives].
Gong, ZH; Liu, YS; Wen, Q; Yan, LD; Yu, G, 2009)
"Thienorphine is an oripavine with long-lasting antinociceptive effects in mice that are thought to be mediated by mu-opioid receptors. "( Thienorphine: receptor binding and behavioral effects in rhesus monkeys.
Becker, GL; France, CP; Gong, ZH; Li, JX; Traynor, JR, 2007)

Effects

ExcerptReference
"Thienorphine has been demonstrated to be a potent, long-acting partial opioid agonist. "( Deep understanding of the interaction between thienorphine and UDP-glucuronosyltransferase (UGT) isoforms.
Cao, YF; Dong, RH; Fang, ZZ; Ge, GB; Hu, CM; Li, XB; Liu, ZY; Xia, YL; Yang, L; Zhu, LL, 2013)

Treatment

ExcerptReference
"Treatment with thienorphine for 24, 48, and 72 h downregulated surface μ-receptor in a dose- and time-dependent manner."( Multiple mechanisms underlying the long duration of action of thienorphine, a novel partial opioid agonist for the treatment of addiction.
Cui, MX; Gong, ZH; Li, SH; Su, RB; Yan, LD; Yong, Z; Yu, G; Zhou, PL, 2014)

Pharmacokinetics

ExcerptReference
" Pharmacokinetic data of thienorphine and its metabolite thienorphine glucuronide conjugate obtained with this method following a single oral dose of 3mg/kg thienorphine to rats were also reported for the first time."( Simultaneous determination of thienorphine and its active metabolite thienorphine glucuronide in rat plasma by liquid chromatography-tandem mass spectrometry and its application to pharmacokinetic studies.
Gong, Z; Kong, Q; Qiao, J; Ruan, J; Wang, X; Yuan, S; Zhang, Z, 2007)

Bioavailability

Thienorphine was a partial opioid agonist with long-lasting antinociceptive effect and high oral bioavailability compared with its analogue buprenorphine.

ExcerptReference
" Additionally, the bioavailability of thienorphine was greatly higher than that of buprenorphine after oral administration."( Thienorphine is a potent long-acting partial opioid agonist: a comparative study with buprenorphine.
Cui, MX; Gong, ZH; Yu, G; Yue, YJ, 2006)
" Thienorphine was a partial opioid agonist with long-lasting antinociceptive effect and high oral bioavailability compared with its analogue buprenorphine."( Effect of thienorphine on the isolated uterine strips from pregnant rats.
Dong, H; Gong, Z; Su, R; Yan, H; Yan, L; Yong, Z; Yu, G; Zhou, P, 2013)
" However, their negative surface charge decreases bioavailability under oral administration."( Preparation and in vitro evaluation of thienorphine-loaded PLGA nanoparticles.
Mei, XG; Xie, XY; Yang, Y, 2016)

Dosage Studied

ExcerptReference
" In the hot plate test and tail-flick test, thienorphine presented the typical partial opioid agonist character with a ceiling dose-response curve in addition to a bell-shaped curve."( Thienorphine induces antinociception without dependence through activation of κ- and δ-, and partial activation of μ- opioid receptor.
Chen, M; Gong, Z; Li, Y; Su, R; Yong, Z; Zhang, Y; Zhou, P, 2020)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (19.05)29.6817
2010's16 (76.19)24.3611
2020's1 (4.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
3,4-dihydroxyphenylacetic acid
3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.. (3,4-dihydroxyphenyl)acetic acid : A dihydroxyphenylacetic acid having the two hydroxy substituents located at the 3- and 4-positions. It is a metabolite of dopamine.. dihydroxyphenylacetic acid : A dihydroxy monocarboxylic acid consisting of phenylacetic acid having two phenolic hydroxy substituents.		2.0710catechols;
dihydroxyphenylacetic acid		human metabolite
lactic acid
Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.		2.77302-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
potassium chloride
Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.		2.1310inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer
betadex
beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.		2.0710cyclodextrin
buprenorphine
Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.. buprenorphine : A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain.		9.47210morphinane alkaloiddelta-opioid receptor antagonist;
kappa-opioid receptor antagonist;
mu-opioid receptor agonist;
opioid analgesic
u-50488
3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer: A non-peptide, kappa-opioid receptor agonist which has also been found to stimulate the release of adrenocorticotropin (ADRENOCORTICOTROPIC HORMONE) via the release of hypothalamic arginine vasopressin (ARGININE VASOPRESSIN) and CORTICOTROPIN-RELEASING HORMONE. (From J Pharmacol Exp Ther 1997;280(1):416-21). U50488 : A monocarboxylic acid amide obtained by formal condensation between the carboxy group of 3,4-dichlorophenylacetic acid and the secondary amino group of (1R,2R)-N-methyl-2-(pyrrolidin-1-yl)cyclohexanamine		2.0310dichlorobenzene;
monocarboxylic acid amide;
N-alkylpyrrolidine		analgesic;
antitussive;
calcium channel blocker;
diuretic;
kappa-opioid receptor agonist
hymecromone
Hymecromone: A coumarin derivative possessing properties as a spasmolytic, choleretic and light-protective agent. It is also used in ANALYTICAL CHEMISTRY TECHNIQUES for the determination of NITRIC ACID.		2.0810hydroxycoumarinantineoplastic agent;
hyaluronic acid synthesis inhibitor
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.		2.4820morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
morphine
Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.		2.9940morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
thebaine
Thebaine: A drug that is derived from opium, which contains from 0.3-1.5% thebaine depending on its origin. It produces strychnine-like convulsions rather than narcosis. It may be habit-forming and is a controlled substance (opiate) listed in the U.S. Code of Federal Regulations, Title 21 Part 1308.12 (1985). (From Merck Index, 11th ed)		2.0610morphinane alkaloid;
organic heteropentacyclic compound
naltrexone
Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.		2.0310cyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound		antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
oripavine
oripavine: from, Papaver orientale L. & P. bacterium Lindl; structure in Merck Index, 9th ed, #6707; RN given refers to (5alpha)-isomer. oripavine : A morphinane alkaloid with formula C18H19NO3. It is the major metabolite of thebaine.		2.0610ether;
morphinane alkaloid;
organic heteropentacyclic compound;
organic hydroxy compound;
tertiary amino compound		bacterial xenobiotic metabolite;
opioid analgesic
heptakis(2,6-o-dimethyl)beta-cyclodextrin
heptakis(2,6-O-dimethyl)beta-cyclodextrin: stimulant for Bordetella pertussis Phase I		2.0710
chitosan
[no description available]		2.1310
ConditionIndicatedRelationship StrengthStudiesTrials
Ache
[description not available]		02.2510
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		02.2510
Addiction, Opioid
[description not available]		02.0810
Opioid-Related Disorders
Disorders related to or resulting from abuse or misuse of OPIOIDS.		02.0810
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.0810
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		03.0240
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.110
Morphine Abuse
[description not available]		02.110
Morphine Dependence
Strong dependence, both physiological and emotional, upon morphine.		02.110
Drug Withdrawal Symptoms
[description not available]		02.0710
Substance Withdrawal Syndrome
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.		02.0710
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0310