methocinnamox

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

Description

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

Cross-References

ID Source	ID
PubMed CID	46877713
CHEMBL ID	610884
MeSH ID	M0369159

Synonyms (6)

Synonym
CHEMBL610884
mcam
methocinnamox
117339-76-1
(e)-n-[(4r,4as,7ar,12br)-3-(cyclopropylmethyl)-9-hydroxy-7-oxo-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-4a-yl]-3-(4-methylphenyl)prop-2-enamide
GLXC-25817

Research Excerpts

Overview

Methocinnamox (MCAM) is a novel, long-acting opioid receptor antagonist. MCAM might be an effective treatment for opioid use disorder.

Excerpt	Reference	Relevance
"Methocinnamox (MCAM) is a novel, long-acting opioid receptor antagonist that might be an effective treatment for opioid use disorder (i.e., preventing relapse and overdose)."	( Daily methocinnamox treatment dose-dependently attenuates fentanyl self-administration in rhesus monkeys. France, CP; Maguire, DR, 2024)	2.64

Dosage Studied

Excerpt	Relevance	Reference
"8 mg/kg) produced a 74-fold increase in the ED(50) of morphine while showing no effect on bremazocine or BW373U86 dose-response curves."	( Methocinnamox is a potent, long-lasting, and selective antagonist of morphine-mediated antinociception in the mouse: comparison with clocinnamox, beta-funaltrexamine, and beta-chlornaltrexamine. Broadbear, JH; Burke, TF; Husbands, SM; Lewis, JW; Sumpter, TL; Traynor, JR; Woods, JH, 2000)	1.75

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

Bioassays (7)

Assay ID	Title	Year	Journal	Article
AID269592	Antagonist activity against morphine-induced antinociception in sc dosed mouse by tail flick assay	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID269588	Agonist activity in sc dosed mouse by phenylquinone abdominal stretching assay	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID269587	Agonist activity in sc dosed mouse by tail flick assay	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID269594	Agonist activity in mouse by hot water tail withdrawal assay at 32 mg/kg, sc	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID269597	Antagonist activity against morphine-induced antinociception in sc dosed mouse by hot water tail withdrawal assay at 32 mg/kg, sc	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID1054689	Selectivity ratio of Ki for human delta opioid receptor to Ki for human mu opioid receptor	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID1054688	Selectivity ratio of Ki for human kappa opioid receptor to Ki for human mu opioid receptor	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	3 (27.27)	29.6817
2010's	2 (18.18)	24.3611
2020's	6 (54.55)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.92

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 moderate demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	25.92 (24.57)
Research Supply Index	2.48 (2.92)
Research Growth Index	5.07 (4.65)
Search Engine Demand Index	26.67 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (25.92)

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
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.	3.04	3	anilide; monocarboxylic acid amide; piperidines	adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; 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.	2.55	2	morphinane 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.	2.95	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
beta-funaltrexamine beta-funaltrexamine: RN given refers to parent cpd(E)-isomer; structure given in first source	7	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.	3.17	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.	2.49	2
chlornaltrexamine chlornaltrexamine: RN given refers to (5alpha,6beta)-isomer	7	1
cyprodime cyprodime: RN & structure given in first source; RN given refers to parent cpd	2.08	1
clocinnamox clocinnamox: structure given in first source; an opioid mu receptor agonist	7.42	2
guanosine 5'-o-(3-thiotriphosphate) Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.	2	1	nucleoside triphosphate analogue

Condition	Relationship Strength	Studies
Opiate Overdose Accidental or deliberate use of an OPIOID in excess of normal dosage. It includes overdose for prescription and illicit opioids.	3.19	2
Addiction, Opioid [description not available]	2.6	1
Opioid-Related Disorders Disorders related to or resulting from abuse or misuse of OPIOIDS.	2.6	1
Ache [description not available]	2.02	1
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	2.02	1

chemdatabank.com