Page last updated: 2024-12-11

lergotrile

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

Description

lergotrile: RN given refers to parent cpd(8beta)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6918447
CHEMBL ID80937
CHEBI ID177579
SCHEMBL ID635242
MeSH IDM0099843

Synonyms (31)

Synonym
CHEMBL80937
CHEBI:177579
2-[(6ar,9s,10ar)-5-chloro-7-methyl-6,6a,8,9,10,10a-hexahydro-4h-indolo[4,3-g]quinolin-9-yl]acetonitrile
gtpl270
2-[(6ar,9s,10ar)-5-chloro-7-methyl-6,6a,8,9,10,10a-hexahydro-4h-indolo[4,3-fg]quinoline-9-yl]acetonitrile
lergotrile
lergotrilo [inn-spanish]
lergotrilum [inn-latin]
ly 79907
lergotrile [usan:inn]
2-chloro-6-methylergoline-8beta-acetonitrile
ergoline-8-acetonitrile, 2-chloro-6-methyl-, (8beta)-
lergotrile (usan/inn)
36945-03-6
D04693
lergotrilo
unii-o68jxu1w09
lergotrilum
o68jxu1w09 ,
lergotrile [inn]
lergotrile [usan]
ergoline-8-acetonitrile, 2-chloro-6-methyl-, (8.beta.)-
SCHEMBL635242
JKAHWGPTNVUTNB-IXPVHAAZSA-N
2-[(6ar,9s,10ar)-5-chloro-7-methyl-6,6a,8,9,10,10a-hexahydro-4h-indolo[4,3-fg]quinolin-9-yl]acetonitrile
Q27079974
bdbm50224035
2-((6ar,9s,10ar)-5-chloro-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinolin-9-yl)acetonitrile
lergo; lergotril
DTXSID701043282
AKOS040747043

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Seven DA agonists produced U-shaped dose-response curves indicative of activity at both the autoreceptor and postsynaptic DA receptor."( Mouse locomotor activity: an in vivo test for dopamine autoreceptor activation.
Bendesky, RJ; Martin, GE, 1984
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
organic heterotetracyclic compound
organonitrogen heterocyclic compoundAny organonitrogen compound containing a cyclic component with nitrogen and at least one other element as ring member atoms.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (42)

Assay IDTitleYearJournalArticle
AID47762Compound was tested for percentage decrease in heart rate at 100 mg/kg in anaesthetized cat1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID47766Compound was tested for percentage decrease in heart rate at 30 mg/kg in anaesthetized cat1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID48531Compound was tested for neuronal inhibition of postganglionic cardio accelerator nerve stimulation in anaesthetized cat at 2 Hz frequency at 300 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID1147971Inhibition of ovum implantation in sc dosed inseminated rat1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Ergot alkaloids. New ergolines as selective dopaminergic stimulants.
AID47949Compound tested in vitro for sympathetic neuronal activity in cat atria after iv administration; not tested1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
6-Hydroxy-4-[2-(di-n-propylamino)ethyl]indole: synthesis and dopaminergic actions.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID62448Inhibitory binding activity against dopamine receptor using [3H]ADTN as the radioligand in striatal tissue of calf brain.1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Conformationally restricted congeners of dopamine derived from 2-aminoindan.
AID1147967Induction of turning toward intact side in OFA rat model with 6-OH-DA-induced unilateral degeneration of nigrostriatal tract at 1 mg/kg, ip1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Ergot alkaloids. New ergolines as selective dopaminergic stimulants.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID48532Compound was tested for neuronal inhibition of postganglionic cardio accelerator nerve stimulation in anaesthetized cat at 2 Hz frequency at 30 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID48542Compound was tested for inhibitory effect reversed by haloperidol (100 ug/kg) at 30 mg/kg in anaesthetized cat; Yes1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID62450Inhibitory binding activity against dopamine receptor using [3H]spiperone as the radioligand in striatal tissue of calf brain.1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Conformationally restricted congeners of dopamine derived from 2-aminoindan.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID47768Compound was tested for percentage decrease in mean arterial blood pressure at 100 mg/kg in anaesthetized cat1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID48889Potency relative to apomorphine at 30 mg/kg in anaesthetized cat1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1123660Inhibition of prolactin release in rat at 10 ug relative to control1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Ergot alkaloids. Synthesis of nitrosourea derivatives of ergolines as potential anticancer agents.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID47951Compound tested in vivo for sympathetic neuronal activity in cat cardioaccelerator nerve after iv administration1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
6-Hydroxy-4-[2-(di-n-propylamino)ethyl]indole: synthesis and dopaminergic actions.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID47771Compound was tested for percentage decrease in mean arterial blood pressure at 300 mg/kg in anaesthetized cat1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1147968Induction of stereotypy in OFA rat at 30 mg/kg, ip measured every 30 mins for 2 hrs followed by every 60 mins for 7 hrs1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Ergot alkaloids. New ergolines as selective dopaminergic stimulants.
AID48367The compounds were evaluated for their ability to inhibit the positive chronotropic effect of stimulation of the cardioaccelerator nerve in the anesthetized cat1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Conformationally restricted congeners of dopamine derived from 2-aminoindan.
AID48529Compound was tested for neuronal inhibition of postganglionic cardio accelerator nerve stimulation in anaesthetized cat at 2 Hz frequency at 100 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID48360Sympathetic neuronal inhibiting activity in anaesthetized cat at 30 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1147970Inhibition of serum prolactin in sc dosed rat after 4 hrs by RIA1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Ergot alkaloids. New ergolines as selective dopaminergic stimulants.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID47765Compound was tested for percentage decrease in heart rate at 300 mg/kg in anaesthetized cat1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID47772Compound was tested for percentage decrease in mean arterial blood pressure at 30 mg/kg in anaesthetized cat1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-199027 (96.43)18.7374
1990's1 (3.57)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)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: 18.49

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.

MetricThis Compound (vs All)
Research Demand Index18.49 (24.57)
Research Supply Index3.40 (2.92)
Research Growth Index4.26 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (6.90%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (93.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]