Page last updated: 2024-12-10
l 366509
Description
L 366509: oxytocin antagonist; considered for treatment of preterm labor; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
Synonyms (5)
| Synonym |
|---|
| 138382-23-7 |
| l 366509 |
| CHEMBL339681 , |
| bdbm50001352 |
| 2-[2-hydroxy-7,7-dimethyl-1-spiro[1h-indene-1,4''-(hexahydropyridine)]-1-ylsulfonylmethylbicyclo[2.2.1]hept-2-yl]acetic acid |
Research Excerpts
Bioavailability
| Excerpt | Reference | Relevance |
|---|
| " Derivatives of the spiroindenepiperidine ring system, these compounds include L-366,509, an orally bioavailable OT antagonist with good in vivo duration." | ( Orally active, nonpeptide oxytocin antagonists.
DiPardo, RM; Evans, BE; Gilbert, KF; Gould, NP; Hobbs, DW; Leighton, JL; Lundell, GF; Pettibone, DJ; Rittle, KE; Veber, DF, 1992) | 0.28 |
| " The new OT antagonist L-367,773 (35) is shown to be an orally bioavailable agent with good duration in vivo and to inhibit OT-stimulated uterine contractions effectively in several in vitro and in vivo models." | ( Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
Bock, MG; Carroll, LA; Evans, BE; Gilbert, KF; Leighton, JL; Lundell, GF; Pawluczyk, JM; Rittle, KE; Williams, PD; Young, MB, 1993) | 0.29 |
Protein Targets (1)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|
| Oxytocin receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.7800 | 0.0089 | 0.2992 | 0.7800 | AID151812 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Bioassays (3)
| Assay ID | Title | Year | Journal | Article |
|---|
| AID213759 | Half-maximal inhibition of binding of [3H]vasopressin to vasopressin receptor 1 in rat liver | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Orally active, nonpeptide oxytocin antagonists. |
| AID213929 | Half-maximal inhibition of binding of [3H]- vasopressin to the vasopressin receptor 2 in rat kidney | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Orally active, nonpeptide oxytocin antagonists. |
| AID151812 | Half-maximal inhibition of binding of [3H]oxytocin to OT receptor in rat uterine tissue | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Orally active, nonpeptide oxytocin antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (80.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 1 (20.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |