oxymorphazone

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

Description

oxymorphazone: binds irreversibly to opiate receptor sites; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	5490705
CHEMBL ID	351916
MeSH ID	M0106643

Synonyms (4)

Synonym
oxymorphazone
CHEMBL351916
(4r,4as,7z,7ar,12bs)-7-hydrazinylidene-3-methyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol
Q7116020

Research Excerpts

Overview

Oxymorphazone is a 14-hydroxydihydromorphinone derivative which contains a C-6 hydrazone group. It could serve as an irreversible label for opioid receptors.

Excerpt	Reference	Relevance
"Oxymorphazone is a 14-hydroxydihydromorphinone derivative which contains a C-6 hydrazone group and hence could serve as an irreversible label for opioid receptors. "	( Synthesis and binding of 3H-oxymorphazone to rat brain membranes. Benyhe, S; Borsodi, A; Hosztafi, S; Toth, G; Varga, E, 1987)	2.01
"Oxymorphazone is a 14-hydroxydihydromorphinone derivative which contains C-6 hydrazone group and hence could serve as an irreversible label for opioid receptors. "	( Preparation of [3H]-oxymorphazone and its binding to rat brain membranes. Borsodi, A; Hosztafi, S; Toth, G; Varga, E, 1986)	2.04

Dosage Studied

Excerpt	Relevance	Reference
" Dose-response curves at 1 hr revealed similar potencies of oxymorphone and the derivatives, with the exception of OxyPNPH which was significantly less potent."	( Irreversible opiate agonists and antagonists. IV. Analgesic actions of 14-hydroxydihydromorphinone hydrazones. Bodnar, RJ; Burks, TF; Clark, JE; Hahn, EF; Pasternak, GW; Williams, CL, 1988)	0.27

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

Bioassays (19)

Assay ID	Title	Year	Journal	Article
AID195707	Percent decrease in activity for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of NaCl at dose of 10 nM compared with that of control (6070+/-75 cpm).	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195702	The compound was tested in vitro for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of standard at 4 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195706	Percent decrease in activity for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of NaCl and MnCl2 at dose of 4 nM compared with that of control (5840+/-72 cpm).	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195704	Percent decrease in activity for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of MnCl2 at dose of 4 nM compared with that of control (4080+/-138 cpm).	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195709	Percent decrease in activity for the inhibition of [3H]-Naltrexone in rat brain homogenates in the presence of standard at dose of 10 nM compared with that of control (4930+/-143 cpm).	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID111971	Percent analgesia of compound was measured in mice by using tail-flick assay	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195705	Percent decrease in activity for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of NaCl and MnCl2 at dose of 10 nM compared with that of control (5840+/-72 cpm).	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195694	The ability of compound was measured to replace [3H]-labeled [D-Ala2, Met5]-enkephalinamide in rat brain homogenates by using [3H]-opiate binding assay	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195697	The compound was tested in vitro for the inhibition of [3H]-Naltrexone in rat brain homogenates in the presence of MnCl2 at 4 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195710	Percent decrease in activity for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of standard at dose of 4 nM compared with that of control (4930+/-143 cpm).	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195708	Percent decrease in activity for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of NaCl at dose of 4 nM compared with that of control (6070+/-75 cpm).	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195698	The compound was tested in vitro for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of NaCl and MnCl2 at 10 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195703	Percent decrease in activity for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of MnCl2 at dose of 10 nM compared with that of control (4080+/-138 cpm).	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195712	The compound was tested in vitro for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of NaCl at 4 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195700	The compound was tested in vitro for the inhibition of [3H]-Naltrexone in rat brain homogenates in the presence of NaCl at 10 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID227642	The compound was tested in vitro for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of MnCl2 at 10 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID227644	The compound was tested in vitro for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of standard at 10 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID227643	The compound was tested in vitro for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of NaCl and MnCl2 at 10 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID195699	The compound was tested in vitro for the inhibition of [3H]naltrexone in rat brain homogenates in the presence of NaCl and MnCl2 at 4 nM dose.	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	10 (100.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	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]

Market Indicators

Research Demand Index: 37.21

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	37.21 (24.57)
Research Supply Index	2.48 (2.92)
Research Growth Index	4.45 (4.65)
Search Engine Demand Index	50.49 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (37.21)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
enkephalin, methionine Enkephalin, Methionine: One of the endogenous pentapeptides with morphine-like activity. It differs from LEU-ENKEPHALIN by the amino acid METHIONINE in position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.	1.96	1
enkephalinamide-met, ala(2)- enkephalinamide-Met, Ala(2)-: synthetic enkephalin analog;	1.96	1
enkephalin, leucine Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.. Leu-enkephalin : A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-leucine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide produced in vertebrate species, including rodents, primates and humans that results from decomposition of proenkephalin or dynorphin and exhibits antinociceptive properties.	1.97	1	pentapeptide; peptide zwitterion	analgesic; delta-opioid receptor agonist; human metabolite; mu-opioid receptor agonist; neurotransmitter; rat metabolite
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.	2.37	2	morphinane alkaloid	delta-opioid receptor antagonist; kappa-opioid receptor antagonist; mu-opioid receptor agonist; opioid analgesic
hydromorphone Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class.	3.47	8	morphinane alkaloid; organic heteropentacyclic compound	mu-opioid receptor agonist; opioid analgesic
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.	3.35	7	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
oxymorphone Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)	3.67	10	morphinane alkaloid
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.	2.88	4	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
dihydromorphine Dihydromorphine: A semisynthetic analgesic used in the study of narcotic receptors.	1.96	1	morphinane alkaloid
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.	3.06	5	cyclopropanes; morphinane-like compound; organic heteropentacyclic compound	antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic
enkephalin, ala(2)-mephe(4)-gly(5)- Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.	1.97	1
morphinans Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.	2.37	2	isoquinoline alkaloid fundamental parent; morphinane alkaloid
enkephalin, leucine-2-alanine Enkephalin, Leucine-2-Alanine: A delta-selective opioid (ANALGESICS, OPIOID). It can cause transient depression of mean arterial blood pressure and heart rate.	1.97	1
naloxonazine naloxonazine: binds irreversibly to opiate receptor sites; structure given in first source	1.96	1
naltrexazone naltrexazone: binds irreversibly to opiate receptor sites; structure given in first source	2.36	2
naltrexonazine naltrexonazine: binds irreversibly to opiate receptor sites; structure given in first source	1.96	1
naloxazone naloxazone: has high affinity for opiate receptor binding sites; structure given in first source	2.36	2

Condition	Indicated	Relationship Strength	Studies	Trials
Acute Hypercapnic Respiratory Failure [description not available]	0	1.96	1	0
Respiratory Insufficiency Failure to adequately provide oxygen to cells of the body and to remove excess carbon dioxide from them. (Stedman, 25th ed)	0	1.96	1	0

chemdatabank.com