Page last updated: 2024-12-07

2-ethyl-8-methyl-2,8-diazaspiro(4,5)decane-1,3-dione

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

Description

2-ethyl-8-methyl-2,8-diazaspiro(4,5)decane-1,3-dione: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID87934
CHEMBL ID273308
SCHEMBL ID1043555
MeSH IDM0042284

Synonyms (24)

Synonym
2-ethyl-8-methyl-2,8-diaza-spiro[4.5]decane-1,3-dione (rs-86)
2-ethyl-8-methyl-2,8-diaza-spiro[4.5]decane-1,3-dione
bdbm50038212
2-ethyl-8-methyl-2,8-diaza-spiro[4.5]decane-1,3-dione(rs-86)
3576-73-6
nsc-186065
nsc186065
2,8-diazaspiro(4,5)decane-1,3-dione, 2-ethyl-8-methyl-
2-ethyl-8-methyl-2,8-diazaspiro(4,5)decane-1,3-dione
rs 86
nsc 186065
rs 86hb
CHEMBL273308 ,
AKOS005066367
4m7e1ge80e ,
unii-4m7e1ge80e
2,8-diazaspiro(4.5)decane-1,3-dione, 2-ethyl-8-methyl-
SCHEMBL1043555
rs86
2,8-diazaspiro[4.5]decane-1,3-dione, 2-ethyl-8-methyl-
2,8-diazaspiro[4.5]decane-1,3-dione,2-ethyl-8-methyl-
2-ethyl-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione
Q27260082
DTXSID50897164

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"The centrally active muscarinic agonist RS-86 elicited a dose-dependent anergic-anhedonic syndrome in a double-blind dose-response study in one healthy volunteer."( Endocrine parameters and biogenic amines in relationship to psychopathology after cholinergic drug challenge (RS-86).
Beckmann, H; Fritze, J; Riederer, P; Sofic, E, 1988
)
0.27
" Therefore, the orally active muscarinic agonist RS 86 was tested in a double-blind dose-response study for its psychotropic effects in one healthy volunteer."( The cholinergic agonist RS 86: a pharmacopsychological study.
Beckmann, H; Fritze, J, 1988
)
0.27
" As RS 86, when used in the same dose range, causes a shortening of rapid eye movement (REM) latency and displays antimanic properties, it is unlikely that a reduced dosage of RS 86 in itself accounts for the lack of stimulation of the HPA axis."( The influence of the muscarinic agonist RS 86 on the cortisol system.
Berger, M; Bossert, S; Krieg, JC; Pirke, KM; von Zerssen, D, 1987
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)K app2.16570.00000.98246.2000AID142097; AID142098; AID142209; AID142210
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)K app2.16570.00000.98246.2000AID142097; AID142098; AID142209; AID142210
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)K app2.16570.00000.98246.2000AID142097; AID142098; AID142209; AID142210
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)K app2.16570.00000.98246.2000AID142097; AID142098; AID142209; AID142210
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)K app2.16570.00001.00846.2000AID142097; AID142098; AID142209; AID142210
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID142097In vitro for its ability to displace [3H]NMS from muscarinic acetylcholine receptor in rat cortical homogenates1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Novel quinuclidine-based ligands for the muscarinic cholinergic receptor.
AID142092Apparent binding affinity at v, by displacing [3H]N-methylscopolamine (NMS) in rat cortex1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
2-Methyl-1,3-dioxaazaspiro[4.5]decanes as novel muscarinic cholinergic agonists.
AID231289Ratio of binding affinity at [3H]quinuclidinyl benzilate binding on rat brain stem homogenate to [3H]-Piperazine binding on rat brain homogenate1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID231288Ratio of binding affinity at [3H]quinuclidinyl benzilate binding on rat brain homogenate to [3H]- Oxotremorine-M binding on rat brain homogenate1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID140993M2/M3 agonist activity estimated by contraction of isolated guinea pig ileum1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID142724In vitro binding affinity for muscarinic M1 receptor by displacing [3H]pirenzepine binding on rat brain homogenate.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID230246Ratio of NMS/oxo-M apparent binding affinities (Kapp)1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
2-Methyl-1,3-dioxaazaspiro[4.5]decanes as novel muscarinic cholinergic agonists.
AID141091In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidinyl benzilate binding on rat brain stem homogenate.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID232606Ratio of IC50 QNB to that of OXO-M was determined1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.
AID112706Dose producing 50% fall in rhythmic slow wave activity in mouse1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.
AID142613M1 agonist activity estimated by rat superior cervical ganglion depolarization1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID142089Apparent binding affinity at Muscarinic acetylcholine receptor by displacing [3H]oxotremorine-M in rat cortex1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
2-Methyl-1,3-dioxaazaspiro[4.5]decanes as novel muscarinic cholinergic agonists.
AID112393Tremorigenic effects were assessed in mice after subcutaneous administration of the compound1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.
AID142859In vivo determination of peripheral M2 receptor mediated hypothermia, cholinergic side effect1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID141094In vitro binding affinity for muscarinic receptor by displacing [3H]oxotremorine-M binding on rat brain homogenate.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID142740M2 agonist activity estimated by depression of isolated guinea pig left atrium1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID142369The selectivity ratio of Kapp of NMS/OXO -M1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors.
AID142098In vitro displacement of [3H]OXO-M from muscarinic acetylcholine receptor in rat cortical homogenates1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Novel quinuclidine-based ligands for the muscarinic cholinergic receptor.
AID142861In vivo determination of peripheral M2 receptor mediated salivation, cholinergic side effect1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID140986In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidinyl benzilate binding on rat brain homogenate1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID142210In vitro binding affinity against muscarinic acetylcholine receptor from rat cortical homogenates using [3H]oxotremorine-M radioligand1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors.
AID233564The ratio of Kapp([3H]-NMS) / Kapp([3H]-OXO-M) was determined1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Novel quinuclidine-based ligands for the muscarinic cholinergic receptor.
AID142862In vivo determination of peripheral M2 receptor mediated tremor, cholinergic side effect1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
AID110673Extrapyramidal effects was assessed from the dose producing tremors1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.
AID142209In vitro binding affinity against muscarinic acetylcholine receptor from rat cortical homogenates using [3H]N-methylscopolamine as radioligand1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (69)

TimeframeStudies, This Drug (%)All Drugs %
pre-199030 (43.48)18.7374
1990's32 (46.38)18.2507
2000's6 (8.70)29.6817
2010's1 (1.45)24.3611
2020's0 (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: 9.57

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

MetricThis Compound (vs All)
Research Demand Index9.57 (24.57)
Research Supply Index4.53 (2.92)
Research Growth Index4.11 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.57)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (31.43%)5.53%
Reviews4 (5.71%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other44 (62.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]