4-amino-8-(2-fluoro-6-methoxy-phenyl)-N-propylcinnoline-3-carboxamide: a GABA(A) alpha2,3 receptor modulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 23581869 |
| CHEMBL ID | 1783282 |
| SCHEMBL ID | 1962584 |
| MeSH ID | M0578921 |
| Synonym |
|---|
| CHEMBL1783282 , |
| azd7325 |
| bdbm50418481 |
| 4-amino-8-(2-fluoro-6-methoxy-phenyl)-n-propyl-cinnoline-3-carboxamide |
| 4-amino-8-(2-fluoro-6-methoxy-phenyl)-n-propylcinnoline-3-carboxamide |
| KYDURMHFWXCKMW-UHFFFAOYSA-N , |
| azd 7325 |
| 4-amino-8-(2-fluoro-6-methoxyphenyl)-n-propylcinnoline-3-carboxamide |
| azd-7325 |
| gtpl7712 |
| knm216xouh , |
| unii-knm216xouh |
| 942437-37-8 |
| SCHEMBL1962584 |
| 3-cinnolinecarboxamide, 4-amino-8-(2-fluoro-6-methoxyphenyl)-n-propyl- |
| azd 7325 [who-dd] |
| EX-A3618 |
| DB13994 |
| BS-17902 |
| Q27074785 |
| BCP29554 |
| azd 7325; azd7325 |
| SB17497 |
| mfcd21337369 |
| D81581 |
| CS-0034076 |
| HY-111052 |
| AKOS037649295 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The aims of this analysis were to develop population pharmacokinetic (PPK) models of AZD7325 and midazolam and to assess the induction effect of AZD7325 on CYP3A4 with midazolam as a substrate." | ( Population pharmacokinetic modelling to assess clinical drug-drug interaction between AZD7325 and midazolam. Al-Huniti, N; Lu, Z; Sunzel, M; Xu, H; Zhou, D, 2014) | 0.4 |
| Excerpt | Relevance | Reference |
|---|---|---|
| "2 µm after 10 mg daily dosing to steady-state." | ( A clinical study to assess CYP1A2 and CYP3A4 induction by AZD7325, a selective GABA(A) receptor modulator - an in vitro and in vivo comparison. Desai, D; Grimm, SW; Lin, J; Ribadeneira, MD; Smith, MA; Sunzel, M; Zhou, D, 2012) | 0.38 |
| " Simulations were performed to predict dosing regimens to account for the induction of CYP3A4." | ( Population pharmacokinetic modelling to assess clinical drug-drug interaction between AZD7325 and midazolam. Al-Huniti, N; Lu, Z; Sunzel, M; Xu, H; Zhou, D, 2014) | 0.4 |
| " The model could provide basis for the rational dosing of AZD7325 in clinical practice." | ( Population pharmacokinetic modelling to assess clinical drug-drug interaction between AZD7325 and midazolam. Al-Huniti, N; Lu, Z; Sunzel, M; Xu, H; Zhou, D, 2014) | 0.4 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | Ki | 0.0005 | 0.0000 | 0.2108 | 5.6234 | AID1604529 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Homo sapiens (human) | Ki | 0.0003 | 0.0000 | 0.1881 | 9.0000 | AID601106 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Homo sapiens (human) | Ki | 0.0003 | 0.0001 | 0.2076 | 9.0000 | AID601106 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Homo sapiens (human) | Ki | 0.2300 | 0.0001 | 0.2442 | 5.6234 | AID1604531 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Homo sapiens (human) | Ki | 0.0013 | 0.0001 | 0.2515 | 5.6234 | AID1604530 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Homo sapiens (human) | Ki | 0.0003 | 0.0001 | 0.2401 | 5.6234 | AID1604528; AID601106 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1604577 | In vivo receptor occupancy at GABAA receptor in sc dosed rat brain | |||
| AID601111 | Allosteric modulation of human GABAA alpha3beta3gamma2 receptor expressed in Xenopus laevis oocytes assessed as effect on GABA-induced chloride current at holding potential of -60mV by two-electrode voltage-clamp electrophysiology assay relative to 1 uM D | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Development and SAR of functionally selective allosteric modulators of GABAA receptors. |
| AID1604528 | Binding affinity to GABA-A alpha2 (unknown origin) | |||
| AID601106 | Displacement of [3H]flunitrazepam from benzodiazepine binding site GABAA alpha2beta3gamma2 receptor expressed in Sf9 cells after 1 hr | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Development and SAR of functionally selective allosteric modulators of GABAA receptors. |
| AID1604535 | Binding affinity to GABA-A alpha2 (unknown origin) assessed as increase in induced current relative to control | |||
| AID1604537 | Binding affinity to GABA-A alpha5 (unknown origin) assessed as increase in induced current relative to control | |||
| AID1604534 | Binding affinity to GABA-A alpha1 (unknown origin) assessed as increase in induced current relative to control | |||
| AID1604530 | Binding affinity to GABA-A alpha3 (unknown origin) | |||
| AID1604531 | Binding affinity to GABA-A alpha5 (unknown origin) | |||
| AID601109 | Allosteric modulation of human GABAA alpha1beta2gamma2 receptor expressed in Xenopus laevis oocytes assessed as effect on GABA-induced chloride current at holding potential of -60mV by two-electrode voltage-clamp electrophysiology assay relative to 1 uM D | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Development and SAR of functionally selective allosteric modulators of GABAA receptors. |
| AID601107 | Solubility of the compound in DMSO by LC/MS/MS method | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Development and SAR of functionally selective allosteric modulators of GABAA receptors. |
| AID1604536 | Binding affinity to GABA-A alpha3 (unknown origin) assessed as increase in induced current relative to control | |||
| AID601110 | Allosteric modulation of human GABAA alpha2beta3gamma2 receptor expressed in Xenopus laevis oocytes assessed as effect on GABA-induced chloride current at holding potential of -60mV by two-electrode voltage-clamp electrophysiology assay relative to 1 uM D | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Development and SAR of functionally selective allosteric modulators of GABAA receptors. |
| AID1604529 | Binding affinity to GABA-A alpha1 (unknown origin) | |||
| AID1604579 | Invivo receptor occupancy GABAA receptor in human assessed as cerebellum concentration causing reduction in [11C]flumazenil receptor labeling at 20 mg by PET method relative to control | |||
| AID601108 | Intrinsic clearance in human liver microsomes at 1 uM after 25 mins by LC/MS/MS analysis in presence of NADPH | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Development and SAR of functionally selective allosteric modulators of GABAA receptors. |
| AID1604578 | Invivo receptor occupancy GABAA receptor in human assessed as occipital cortex concentration causing reduction in [11C]flumazenil receptor labeling at 20 mg by PET method relative to control | |||
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 8 (80.00) | 24.3611 |
| 2020's | 2 (20.00) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (11.84) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (40.00%) | 5.53% |
| Reviews | 1 (10.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (50.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||