quinagolide: structure & RN given in first source; a non-ergot dopamine D(2)-agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 3086401 |
| CHEMBL ID | 290962 |
| CHEBI ID | 135627 |
| SCHEMBL ID | 143485 |
| Synonym |
|---|
| quinagolide (inn/ban) |
| D07217 |
| 87056-78-8 |
| quinagolide |
| CHEBI:135627 |
| CHEMBL290962 |
| (3s,4as,10ar)-3-(diethylsulfamoylamino)-6-hydroxy-1-propyl-3,4,4a,5,10,10a-hexahydro-2h-benzo[g]quinoline |
| SCHEMBL143485 |
| DB09097 |
| Q4860568 |
| bdbm50225362 |
| norprolac;sdz 205-502;cv 205-502 |
| NCGC00522534-01 |
| rel-n,n-diethyl-n'-[(3r,4ar,10as)-1,2,3,4,4a,5,10,10a-octahydro-6-hydroxy-1-propylbenzo[g]quinolin-3-yl]sulfamide |
| 140630-80-4 |
| (3s,4as,10ar)-3-[(diethylsulfamoyl)amino]-1-propyl-1h,2h,3h,4h,4ah,5h,10h,10ah-benzo[g]quinolin-6-ol |
| EN300-18435304 |
Quinagolide (CV 205 502) is a dopamine D2-receptor agonist. It has proved effective in the treatment of prolactinomas, reducing both serum PRL and tumour size. Quinaglide is a nonergot dopamine agonist that is administered once daily.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Quinagolide has a strong dopaminerg activity, suppresses prolactin secretion and restores gonadal function in women with hyperprolactinemic anovulation. " | ( [Treatment of hyperprolactinemic anovulation with the dopamin-agonist quinagolide]. Keresztúri, A; Koloszár, S; Kovács, L, 2000) | 1.98 |
| "Quinagolide has a strong dopaminerg activity, suppresses prolactin secretion and restores gonadal function in women with hyperprolactinemic anovulation. " | ( [Treatment of hyperprolactinemic anovulation with the dopamin-agonist quinagolide]. Keresztúri, A; Koloszár, S; Kovács, L, 2000) | 1.98 |
Quinagolide and CAB treatments, induced the normalization of serum PRL levels in the great majority of patients with prolactinoma. The treatment with quinaglide was carried out at the dose of 0.3-0.6 mg/day for 6-12 months.
| Excerpt | Reference | Relevance |
|---|---|---|
| " In conclusion, we found CV 205-502 effective in one daily dose, with good tolerability; it is safe and provides a valuable alternative to the dopamine agonist drugs in use today." | ( CV 205-502--effectiveness, tolerability, and safety over 24-month study. Homburg, R; Jacobs, HS; Shoham, Z, 1991) | 0.28 |
| " Adverse effects were mild and transient and resolved with dosage manipulation or a divided dosage regimen." | ( CV 205-502: safety, tolerance to, and efficacy of increasing doses in patients with Parkinson's disease in a double-blind, placebo crossover study. Gauger, LL; Olanow, CW; Werner, EG, 1989) | 0.28 |
| " The pooled proportion of adverse effects was 13%, with a 95% confidence interval of 11%-16%." | ( The efficacy and safety of quinagolide in hyperprolactinemia treatment: A systematic review and meta-analysis. Huang, Q; Li, M; Tan, J; Zeng, Y; Zhou, W; Zou, Y, 2023) | 1.21 |
Quinagolide may improve patient compliance to treatment owing to its reduced side effect profile. Simple and rapid titration over just 7 days, once-daily dosing regimen and easy to use starter pack (available in some countries)
| Excerpt | Relevance | Reference |
|---|---|---|
| " The mean integrated GH secretion expressed in arbitrary units [area under the response curve (AUC)] up to 3 h postinfusion showed a typical dose-response relationship." | ( Stimulation of growth hormone release in man by the potent D2-dopamine agonist CV 205-502: comparison of responses to intravenous and oral administration. Corder, R; Gaillard, RC; Miell, JP; Pralong, FP, 1990) | 0.28 |
| " We performed a dosage ranging and placebo crossover study in six patients to evaluate the efficacy and tolerance of CV when used as an adjunct to Sinemet in patients with Parkinson's disease." | ( CV 205-502: safety, tolerance to, and efficacy of increasing doses in patients with Parkinson's disease in a double-blind, placebo crossover study. Gauger, LL; Olanow, CW; Werner, EG, 1989) | 0.28 |
| " Adverse reactions were experienced by 15 patients during dosage increment and caused one patient to discontinue the medication." | ( Long-term treatment of macroprolactinomas with CV 205-502. Bakke, S; Bjøro, T; Brownell, J; Djøseland, O; Halse, J; Hansen, E; Jervell, J; Kvistborg, A, 1993) | 0.29 |
| " The dosage of quinagolide ranged from 75 to 400 [mgr]g/day with a median dose of 100[mgr]g/day." | ( Quinagolide in the management of prolactinoma. Gagel, RF; Ginsberg, L; Leavens, M; McCutcheon, IE; Samaan, N; Schultz, PN, 2000) | 2.1 |
| " However, bromocriptine requires multiple daily dosing and some patients are resistant or intolerant to this therapy." | ( Current treatment issues in female hyperprolactinaemia. Crosignani, PG, 2006) | 0.33 |
| " Quinagolide may improve patient compliance to treatment owing to its reduced side effect profile, simple and rapid titration over just 7 days, once-daily dosing regimen and easy to use starter pack (available in some countries)." | ( Quinagolide--a valuable treatment option for hyperprolactinaemia. Barlier, A; Jaquet, P, 2006) | 2.69 |
| " The psychotic symptoms started after a dosage increase of a dopamine D2-receptor agonist." | ( Treating prolactinoma and psychosis: medication and cognitive behavioural therapy. Becker, HE; Birchwood, M; de Haan, L; Drent, ML; Nieman, DH; Otten, J; Sutterland, AL; van der Gaag, M, 2011) | 0.37 |
| Class | Description |
|---|---|
| organonitrogen heterocyclic compound | Any organonitrogen compound containing a cyclic component with nitrogen and at least one other element as ring member atoms. |
| organic heterotricyclic compound | An organic tricyclic compound in which at least one of the rings of the tricyclic skeleton contains one or more heteroatoms. |
| [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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0004 | 0.6298 | 10.0000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0004 | 0.9086 | 10.0000 | AID203936; AID203937 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 7.9333 | 0.0002 | 1.8742 | 10.0000 | AID32964 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0003 | 1.3833 | 8.4000 | AID203936; AID203937 |
| D(2) dopamine receptor | Bos taurus (cattle) | IC50 (µMol) | 12.0760 | 0.0010 | 0.7994 | 8.0000 | AID62437; AID62438; AID62439; AID62440; AID62441; AID62442 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 7.9333 | 0.0002 | 1.2704 | 10.0000 | AID32964 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0005 | 1.4835 | 7.8000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0031 | 1.7360 | 7.8000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 1F | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0050 | 1.7962 | 7.8000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0004 | 0.6156 | 10.0000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 6 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0050 | 1.5089 | 4.6000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 7 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0050 | 1.4282 | 4.6000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 5A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0050 | 1.3598 | 4.6000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 5B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0050 | 1.3598 | 4.6000 | AID203936; AID203937 |
| 5-hydroxytryptamine receptor 3A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0002 | 1.1351 | 4.6000 | AID203936; AID203937 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 7.9333 | 0.0000 | 1.8194 | 10.0000 | AID32964 |
| 5-hydroxytryptamine receptor 4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 6.4800 | 0.0050 | 1.3552 | 4.6000 | AID203936; AID203937; AID62440 |
| D | Bos taurus (cattle) | IC50 (µMol) | 12.0760 | 0.0010 | 0.4720 | 8.0000 | AID62437; AID62438; AID62439; AID62440; AID62441; AID62442 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | IC50 (µMol) | 4.6000 | 0.0003 | 0.7028 | 5.3660 | AID203936 |
| 5-hydroxytryptamine receptor 3B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.6000 | 0.0004 | 1.1742 | 4.6000 | AID203936; AID203937 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| G protein-coupled opioid receptor activity | Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) |
| protein binding | Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID36920 | In vitro inhibitory activity was evaluated against,[3H]clonidine (Clon) rat brain minus cerebellum Alpha-2 adrenergic receptor | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID62442 | In vitro inhibitory activity was evaluated against,[3H]spiperone calf caudate (SPC) dopamine receptor | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID203938 | In vitro inhibitory activity was evaluated against,[3H]spiperone rat frontal cortex (SPFC) serotonin receptor | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID36861 | In vitro inhibitory activity against alpha-1 adrenergic receptor from whole rat brain using [3H]WB-4101 as radioligand | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| AID182642 | Compound was evaluated for the in vivo inhibition of basal prolactin for a time 4 hr after injection in male rats | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID62437 | In vitro inhibitory activity against dopamine receptor from calf caudate using [3H]dopamine as radioligand | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| AID62441 | In vitro inhibitory activity was evaluated against,[3H]dopamine (DA),calf caudate dopamine receptor | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID62440 | In vitro inhibitory activity was evaluated against [3H]spiperone calf caudate (SPC) dopamine receptor | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID182644 | Compound was evaluated for the in vivo inhibition of basal prolactin secretion for a time 4 hr after injection in male rats | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID182954 | In vivo inhibitory against lactation in female rat after peroral administration | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| AID203937 | In vitro inhibitory activity was evaluated against,[3H]serotonin (5-HT) whole rat brain serotonin receptor | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID62439 | In vitro inhibitory activity was evaluated against [3H]dopamine (DA) calf caudate dopamine receptor | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID203935 | In vitro inhibitory activity against serotonin receptor from rat frontal cortex using [3H]spiperone as radioligand | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| AID32964 | In vitro inhibitory activity was evaluated against,[3H]WB 4101 whole rat brain alpha 1-adrenoceptor | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide. |
| AID62438 | In vitro inhibitory activity against dopamine receptor from calf caudate using [3H]spiperone as radioligand | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| AID182951 | In vivo inhibitory activity against ovum implantation in female rat after subcutaneous administration | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| AID182949 | In vivo inhibitory activity against basal prolactin in male rat after subcutaneous administration | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| AID203936 | In vitro inhibitory activity against serotonin receptor from whole rat brain using [3H]5-HT as radioligand | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| AID36919 | In vitro inhibitory activity against alpha-2 adrenergic receptor from rat brain minus cerebellum using [3H]clonidine as radioligand | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 18 (9.78) | 18.7374 |
| 1990's | 87 (47.28) | 18.2507 |
| 2000's | 40 (21.74) | 29.6817 |
| 2010's | 34 (18.48) | 24.3611 |
| 2020's | 5 (2.72) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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.
| This Compound (44.24) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 43 (22.40%) | 5.53% |
| Reviews | 27 (14.06%) | 6.00% |
| Case Studies | 27 (14.06%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 95 (49.48%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||