Page last updated: 2024-08-07 16:54:51
Oxytocin receptor
An oxytocin receptor that is encoded in the genome of rat. [OMA:P70536, PRO:DNx]
Synonyms
OT-R
Research
Bioassay Publications (18)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (38.89) | 18.2507 |
| 2000's | 8 (44.44) | 29.6817 |
| 2010's | 3 (16.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (13)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| opc 21268 | Rattus norvegicus (Norway rat) | Ki | 0.2300 | 1 | 1 |
| conivaptan | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| oxytocin | Rattus norvegicus (Norway rat) | Ki | 0.0013 | 2 | 2 |
| arginine vasopressin | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 1 | 1 |
| atosiban | Rattus norvegicus (Norway rat) | IC50 | 0.0120 | 1 | 1 |
| atosiban | Rattus norvegicus (Norway rat) | Ki | 0.0579 | 2 | 2 |
| l 372662 | Rattus norvegicus (Norway rat) | Ki | 0.0150 | 1 | 1 |
| way-151932 | Rattus norvegicus (Norway rat) | IC50 | 0.0550 | 1 | 1 |
| l 371257 | Rattus norvegicus (Norway rat) | IC50 | 0.6400 | 1 | 1 |
| l 371257 | Rattus norvegicus (Norway rat) | Ki | 0.0190 | 3 | 3 |
| l 368899 | Rattus norvegicus (Norway rat) | IC50 | 0.0089 | 1 | 1 |
| deaminooxytocin | Rattus norvegicus (Norway rat) | Ki | 0.0020 | 2 | 2 |
| l 366509 | Rattus norvegicus (Norway rat) | IC50 | 0.7800 | 1 | 1 |
| obe001 | Rattus norvegicus (Norway rat) | Ki | 0.2100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| isoproterenol | Rattus norvegicus (Norway rat) | EC50 | 0.0030 | 1 | 1 |
| atosiban | Rattus norvegicus (Norway rat) | Kd | 1,000,000.0000 | 1 | 1 |
| deaminooxytocin | Rattus norvegicus (Norway rat) | Kd | 1,000,000.0000 | 1 | 1 |
Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.European journal of medicinal chemistry, , Volume: 42, Issue:6, 2007
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.Bioorganic & medicinal chemistry letters, , May-20, Volume: 12, Issue:10, 2002
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.Journal of medicinal chemistry, , Nov-10, Volume: 38, Issue:23, 1995
Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.European journal of medicinal chemistry, , Volume: 42, Issue:6, 2007
A study of the relationship between biological activity and prolyl amide isomer geometry in oxytocin using 5-tert-butylproline to augment the Cys(6)-Pro(7) amide cis-isomer population.Journal of medicinal chemistry, , Apr-20, Volume: 43, Issue:8, 2000
Synthesis and pharmacology of novel analogues of oxytocin and deaminooxytocin: directed methods for the construction of disulfide and trisulfide bridges in peptides.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997