Page last updated: 2024-12-08
ocinaplon
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
ocinaplon: pyrazolo[1,5-a]-pyrimidine that exhibits an anxioselective profile in both preclinical procedures and in patients with generalized anxiety disorder; GABA(A) receptor modulator & Anti-Anxiety Agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 216456 |
| CHEMBL ID | 2105199 |
| SCHEMBL ID | 122652 |
| MeSH ID | M0486834 |
Synonyms (37)
| Synonym |
|---|
| 96604-21-6 |
| ocinaplon (usan/inn) |
| D02617 |
| cl 273547 |
| ocinaplon |
| 2-pyridyl 7-(4-pyridyl)pyrazolo(1,5-a)pyrimidin-3-yl ketone |
| 2-pyridinyl(7-(4-pyridinyl)pyrazolo(1,5-a)pyrimidin-3-yl)methanone |
| methanone, 2-pyridinyl(7-(4-pyridinyl)pyrazolo(1,5-a)pyrimidin-3-yl)- |
| ocinaplon [usan:inn] |
| pyridin-2-yl-(7-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-3-yl)methanone |
| pyridin-2-yl-[7-pyridin-4-yl-pyrazole[1,5-a]pyrimidin-3-yl]methanone |
| cl-273547 |
| CHEMBL2105199 |
| methanone, 2-pyri(dinyl(7-(4-pyridinyl)pyrazolo(1,5-a)pyrimidin-3-yl)- |
| 2h6kvc5e76 , |
| cl 273,547 |
| unii-2h6kvc5e76 |
| gtpl4277 |
| 4-{3-[(pyridin-2-yl)carbonyl]pyrazolo[1,5-a]pyrimidin-7-yl}pyridine |
| 2-pyridyl 7-(4-pyridyl)pyrazolo[1,5-a]pyrimidin-3-yl ketone |
| ocinaplon [usan] |
| ocinaplon [inn] |
| SCHEMBL122652 |
| 2-pyridinyl[7-(4-pyridinyl)pyrazolo[1,5-a]pyrimidin-3-yl]methanone |
| AKOS024458146 |
| DTXSID00242362 |
| CS-W001692 |
| 4-[3-(pyridine-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]pyridine |
| AS-72567 |
| NCGC00370957-01 |
| FT-0762986 |
| pyridin-2-yl(7-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl)methanone |
| DB06529 |
| Q2013712 |
| methanone, 2-pyridinyl[7-(4-pyridinyl)pyrazolo[1,5-a]pyrimidin-3-yl]- |
| HY-W001692 |
| WDA60421 |
Research Excerpts
Overview
Ocinaplon appears to be a well-tolerated and effective treatment for GAD.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Ocinaplon appears to be a well-tolerated and effective treatment for GAD." | ( A multicenter, placebo-controlled, double-blind, randomized study of efficacy and safety of ocinaplon (DOV 273,547) in generalized anxiety disorder. Beer, B; Czobor, P; Lippa, A; Skolnick, P, 2010) | 1.3 |
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " The proportion of patients with treatment-emergent adverse events (TEAE) was not statistically significant between ocinaplon and placebo." | ( A multicenter, placebo-controlled, double-blind, randomized study of efficacy and safety of ocinaplon (DOV 273,547) in generalized anxiety disorder. Beer, B; Czobor, P; Lippa, A; Skolnick, P, 2010) | 0.79 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (7)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 21.3174 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 13.4504 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 11.9877 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (45)
Molecular Functions (18)
Ceullar Components (22)
Bioassays (5)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (8)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (25.00) | 29.6817 |
| 2010's | 4 (50.00) | 24.3611 |
| 2020's | 2 (25.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 26.78
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.
| This Compound (26.78) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (25.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (75.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||