Page last updated: 2024-12-11
f 13640
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
befiradol: a selective serotonin 5-HT1A receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9865384 |
| CHEMBL ID | 45305 |
| SCHEMBL ID | 678174 |
| MeSH ID | M0449474 |
Synonyms (33)
| Synonym |
|---|
| nlx-112 |
| CHEMBL45305 , |
| befiradol |
| f-13640 |
| f13640 , |
| L001676 |
| ((3-chloro-4-fluoro-phenyl)-(4-fluoro-4-((5-methyl-pyridin-2-ylmethyl)-amino)-methyl)piperidin-1-yl)-methadone |
| f 13640 |
| bdbm50328639 |
| (3-chloro-4-fluorophenyl)(4-fluoro-4-(((5-methylpyridin-2-yl)methylamino)methyl)piperidin-1-yl)methanone |
| (3-chloro-4-fluoro-phenyl)-(4-fluoro-4-{[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl)-methanone |
| befiradol [inn] |
| 208110-64-9 |
| rat9oha1yh , |
| unii-rat9oha1yh |
| [3h]nlx-112 |
| gtpl3925 |
| (3-chloro-4-fluorophenyl)-[4-fluoro-4-[[(5-methylpyridin-2-yl)methylamino]methyl]piperidin-1-yl]methanone |
| [3h]f13640 |
| SCHEMBL678174 |
| befiradol [who-dd] |
| (3-chloro-4-fluorophenyl)(4-fluoro-4-((((5-methylpyridin-2-yl)methyl)amino)methyl)piperidin-1-yl)methanone |
| AKOS032954037 |
| CS-0003559 |
| HY-14785 |
| Q4880242 |
| nlx-112 hydrochloride |
| DTXSID90943058 |
| f-13640; f13640; f 13640; nlx-112; nlx112; nlx 112 |
| BCP31302 |
| nlx-112; f13640 |
| befiradol (free base) |
| GLXC-15037 |
Research Excerpts
Overview
F 13640 is a newly discovered high-efficacy 5-HT(1A) receptor agonist. It produces exceptional analgesia in animal models of tonic and chronic, nociceptive and neuropathic pains.
| Excerpt | Reference | Relevance |
|---|---|---|
| "F 13640 is a newly discovered high-efficacy 5-HT(1A) receptor agonist that produces exceptional analgesia in animal models of tonic and chronic, nociceptive and neuropathic pains by novel molecular and neuroadaptive mechanisms. " | ( The novel analgesic, F 13640, produces intra- and postoperative analgesia in a rat model of surgical pain. Bardin, L; Colpaert, FC; Degryse, AD; Gomez de Segura, IA; Kiss, I, 2005) | 2.09 |
| "F 13640 is a recently discovered high-efficacy 5-HT1A receptor agonist that has demonstrated robust anti-allodynic efficacy in a rat model of trigeminal neuropathic pain upon acute and continuous administration. " | ( Effects of the combined continuous administration of morphine and the high-efficacy 5-HT1A agonist, F 13640 in a rat model of trigeminal neuropathic pain. Adriaensen, HF; Colpaert, FC; Deseure, KR, 2004) | 1.98 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1 -yl-metha none." | ( Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors. Assié, MB; Bonnaud, B; Cosi, C; Funes, P; Jubault, N; Kleven, M; Koek, W; Vacher, B, 1999) | 0.3 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Dose-response studies indicated that c-Fos protein expression was induced at doses (0." | ( The novel analgesic and high-efficacy 5-HT1A receptor agonist, F 13640 induces c-Fos protein expression in spinal cord dorsal horn neurons. Besson, JM; Buritova, J; Colpaert, F; Tarayre, JP, 2003) | 0.56 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (9)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 0.0010 | 0.0001 | 0.5326 | 10.0000 | AID1854986 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 30.5000 | 0.0000 | 0.6518 | 10.0000 | AID517902; AID517903 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 0.0009 | 0.0001 | 0.7396 | 10.0000 | AID4413 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 2.0000 | 0.0000 | 0.4362 | 10.0000 | AID517905 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.6020 | 10.0000 | AID517904 |
| Cannabinoid receptor 2 | Mus musculus (house mouse) | Ki | 26.0000 | 0.0002 | 0.0797 | 0.7943 | AID517901 |
| 5-hydroxytryptamine receptor 2A | Sus scrofa (pig) | Ki | 23.0000 | 0.0300 | 0.4270 | 0.9000 | AID517900 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Ki | 26.0000 | 0.0005 | 1.2223 | 8.8000 | AID517901 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A1 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0257 | 0.0015 | 2.2057 | 10.0000 | AID3907 |
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | EC50 (µMol) | 0.0246 | 0.0001 | 0.2571 | 8.0000 | AID298093; AID3907 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (133)
Molecular Functions (19)
Ceullar Components (25)
Bioassays (28)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID298095 | Induction of forepaw treading in orally dosed rat after 60 mins | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID517897 | Displacement of [3H]WAY-100635 from 5-HT1A receptor in pig cortex membranes | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID298101 | Half life in human plasma | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID517902 | Displacement of [3H]Spiperone from human dopamine D2 long receptor | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID298100 | Bioavailability in dog | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID176228 | Effective intraperitoneal dose in vivo in rat after 15 mins to induce lower lip retraction | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors. |
| AID298103 | Lipophilicity, log D of the compound | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID517899 | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in pig cortex membranes | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID517906 | Displacement of [3H]Prazosin from adrenergic alpha1 receptor in pig cortex membranes | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID298093 | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID4413 | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat cortex using [3H]8-OH-DPAT as a radioligand | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors. |
| AID298099 | Bioavailability in rat | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID517907 | Displacement of [3H]Prazosin from adrenergic alpha2 receptor in pig cortex membranes | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID517905 | Displacement of [3H]Spiperone from human dopamine D4.4 receptor | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID517904 | Displacement of [3H]Spiperone from human dopamine D3 receptor | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID298102 | Dissociation constant, pKa of the compound | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID176232 | Induction of lower lip retraction in rat 60 min after administration, effective peroral dose determined in vivo | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors. |
| AID517900 | Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID298098 | Antidepressant like activity in orally dosed rat after 60 mins by forced swimming test | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID298092 | Binding affinity to 5HT1A receptor in rat cortex membrane | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID517901 | Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID298094 | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to 5-hydroxytryptamine | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID298097 | Ratio of ED50 for forepaw treading induction in rat to ED50 for flat body posture induction in rat | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID1854986 | Binding affinity to 5-HT1A receptor (unknown origin) assessed as inhibition constant | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors. |
| AID298096 | Induction of flat body posture in orally dosed rat as after 60 mins | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID3907 | In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors. |
| AID517903 | Displacement of [3H]Spiperone from human dopamine D2 short receptor | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 2010 | Naunyn-Schmiedeberg's archives of pharmacology, Oct, Volume: 382, Issue:4 | [(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (42)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (2.38) | 18.2507 |
| 2000's | 18 (42.86) | 29.6817 |
| 2010's | 11 (26.19) | 24.3611 |
| 2020's | 12 (28.57) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 12.21
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 (12.21) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (4.76%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 40 (95.24%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||