Page last updated: 2024-11-06

cy 208-243

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

Description

CY 208-243: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID58144
CHEMBL ID313737
CHEBI ID93399
SCHEMBL ID9364562
MeSH IDM0153929

Synonyms (47)

Synonym
cy-208243
CHEMBL313737
HMS3267H13
cy-208-243
BIOMOL-NT_000032
NCGC00025078-01
tocris-1249
BPBIO1_001225
NCGC00025078-02
4,6,6a,7,8,12b-hexahydro-7-methylindolo(4,3-ab)-phenanthridine
indolo(4,3-ab)phenanthridine, 4,6,6a,7,8,12b-hexahydro-7-methyl-, trans-(-)-
cy 208-243
indolophenanthridine
(6ar,12br)-7-methyl-4,6,6a,7,8,12b-hexahydroindolo[4,3-ab]phenanthridine
100999-26-6
unii-8gj4ur780b
8gj4ur780b ,
cy-208,243
BRD-K79353516-001-01-9
DTXSID9042598
(-)-(6ar,12br)-4,6,6a,7,8,12b-hexahydro-7-methylindolo[4,3-a]phenanthridin
SCHEMBL9364562
AKOS024456489
J-000300
SR-01000597425-1
sr-01000597425
CHEBI:93399
lsm-3788
Q5014909
HMS3676C06
HMS3412C06
BRD-K79353516-001-03-5
cy208-243
(2r,11r)-10-methyl-10,15-diazapentacyclo[11.6.1.02,11.03,8.016,20]icosa-1(20),3,5,7,13,16,18-heptaene
HY-106094
CS-0024842
AT36985
MS-23899
(-)-trans-4,6,6a,7,8,12b-hexahydro-7-methylindolo(4,3-ab)phenanthridine
indolo(4,3-ab)phenanthridine, 4,6,6a,7,8,12b-hexahydro-7-methyl-, (6ar-trans)-
indolo(4,3-ab)phenanthridine, 4,6,6a,7,8,12b-hexahydro-7-methyl-, (6ar,12br)-
4,6,6a,7,8,12b-hexahydro-7-methyl-indolo(4,3-ab)phenanthridine, (6ar-trans)-
cy208243
GLXC-02973
(2r,11r)-10-methyl-10,15-diazapentacyclo[11.6.1.0?,??.0?,?.0??,??]icosa-1(20),3,5,7,13,16,18-heptaene
indolo[4,3-ab]phenanthridine,4,6,6a,7,8,12b-hexahydro-7-methyl-,(6ar,12br)-
GLXC-25866

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" After administering [14C]CY 208-243 intrajejunally, absorption rate was defined as the product of porto-arterial substrate difference and portal venous blood flow."( Quantification of absorption, intestinal and hepatic first pass effect in a chronic dog model.
Bodoky, A; Heberer, M; Lemaire, M; Niederberger, W, 1991
)
0.58

Dosage Studied

ExcerptRelevanceReference
" These experiments provide further evidence that dopaminergic mechanisms may play a role in the regulation of male sexual behavior of rhesus monkeys and, in particular, demonstrate that the direction of the effect depends on the dopamine receptor subtype and dosage of the dopamine agonist being administered."( Dopaminergic influences on male sexual behavior of rhesus monkeys: effects of dopamine agonists.
Pomerantz, SM, 1992
)
0.28
" Simultaneous administration of (+)-PHNO [(+)-4-propyl-9-hydroxynaphthoxazine] and CY 208-243 [(-)4,6,6a,7,8,12b-hexahydro-7-methylindolo[4,3a-b]phenan thyxidine] did not result in modification of the dose-response curve induced by each dopamine receptor agonist given alone."( Functional interaction between dopamine D1 and D2 receptors in 'MPTP' monkeys.
Guillén, J; Laguna, J; Luquin, MR; Martínez-Lage, JM; Martínez-Vila, E, 1994
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
phenanthridinesAny dibenzopyridine based on the skeleton of phenanthridine and its substituted derivatives thereof.
[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]

Protein Targets (43)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency22.47600.003245.467312,589.2998AID2517; AID2572
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency15.84890.004023.8416100.0000AID485290
Chain A, HADH2 proteinHomo sapiens (human)Potency15.84890.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency15.84890.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency10.00000.177814.390939.8107AID2147
15-lipoxygenase, partialHomo sapiens (human)Potency3.16230.012610.691788.5700AID887
phosphopantetheinyl transferaseBacillus subtilisPotency79.43280.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency4.34950.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency10.58430.180013.557439.8107AID1460; AID1468
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency15.84890.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency0.84370.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency12.58930.035520.977089.1251AID504332
runt-related transcription factor 1 isoform AML1bHomo sapiens (human)Potency15.44390.02007.985839.8107AID504370; AID504374; AID504375
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency15.95410.354828.065989.1251AID504847
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency25.11890.010039.53711,122.0200AID1479
core-binding factor subunit beta isoform 2Homo sapiens (human)Potency15.44390.02007.985839.8107AID504370; AID504374; AID504375
mitogen-activated protein kinase 1Homo sapiens (human)Potency15.84890.039816.784239.8107AID995
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency11.22020.00798.23321,122.0200AID2551
DNA polymerase kappa isoform 1Homo sapiens (human)Potency14.12540.031622.3146100.0000AID588579
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency5.01190.031610.279239.8107AID884; AID885
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency26.60860.058010.694926.6086AID588379
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.58930.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency25.11890.01418.602439.8107AID2572
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency25.11890.001551.739315,848.9004AID2572
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency25.11890.01418.602439.8107AID2572
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency25.11890.01418.602439.8107AID2572
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency5.01191.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID464638Selectivity for dopamine D5 receptor over dopamine D1 receptor2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Dopamine receptor ligands. Part 18: (1) modification of the structural skeleton of indolobenzazecine-type dopamine receptor antagonists.
AID61667Tested for its affinity towards Dopamine receptor D1 in rat striatal membrane1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Dopaminergic benzo[a]phenanthridines: resolution and pharmacological evaluation of the enantiomers of dihydrexidine, the full efficacy D1 dopamine receptor agonist.
AID42815In vitro percent maximal stimulation relative to dopamine (125 uM) in bovine retina1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Structure-activity relationships in the trans-hexahydroindolo[4,3-ab]phenanthridine ("benzergoline") series. 2. Resolution, absolute configuration, and dopaminergic activity of the selective D1 agonist CY 208-243 and its implication for an "extended rotam
AID184944Tested in vitro for percent maximal inhibition in rat striatal slices (% of control) expressed as change of S1/S2 versus control at 1 uM1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Structure-activity relationships in the trans-hexahydroindolo[4,3-ab]phenanthridine ("benzergoline") series. 2. Resolution, absolute configuration, and dopaminergic activity of the selective D1 agonist CY 208-243 and its implication for an "extended rotam
AID34165Compound was evaluated for in vitro potency against adenylate cyclase in bovine retina1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Structure-activity relationships in the trans-hexahydroindolo[4,3-ab]phenanthridine ("benzergoline") series. 2. Resolution, absolute configuration, and dopaminergic activity of the selective D1 agonist CY 208-243 and its implication for an "extended rotam
AID34166In vitro potency against adenylate cyclase in bovine retina1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Structure-activity relationships in the trans-hexahydroindolo[4,3-ab]phenanthridine ("benzergoline") series. 2. Resolution, absolute configuration, and dopaminergic activity of the selective D1 agonist CY 208-243 and its implication for an "extended rotam
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (63)

TimeframeStudies, This Drug (%)All Drugs %
pre-199011 (17.46)18.7374
1990's48 (76.19)18.2507
2000's1 (1.59)29.6817
2010's1 (1.59)24.3611
2020's2 (3.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.80

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 Index10.80 (24.57)
Research Supply Index4.19 (2.92)
Research Growth Index4.99 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (3.17%)5.53%
Reviews2 (3.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other59 (93.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]