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Vasopressin V1a receptor
A vasopressin V1a receptor that is encoded in the genome of rat. [OMA:P30560, PRO:DNx]
Synonyms
V1aR;
AVPR V1a;
Antidiuretic hormone receptor 1a;
Vascular/hepatic-type arginine vasopressin receptor
Research
Bioassay Publications (20)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (5.00) | 18.7374 |
| 1990's | 10 (50.00) | 18.2507 |
| 2000's | 5 (25.00) | 29.6817 |
| 2010's | 4 (20.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (13)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| relcovaptan | Rattus norvegicus (Norway rat) | Ki | 0.0014 | 1 | 1 |
| opc 21268 | Rattus norvegicus (Norway rat) | IC50 | 0.4400 | 1 | 1 |
| opc 21268 | Rattus norvegicus (Norway rat) | Ki | 0.0299 | 4 | 4 |
| mozavaptan | Rattus norvegicus (Norway rat) | IC50 | 3.2000 | 2 | 2 |
| lixivaptan | Rattus norvegicus (Norway rat) | IC50 | 0.2930 | 4 | 4 |
| oxytocin | Rattus norvegicus (Norway rat) | Ki | 0.0610 | 1 | 1 |
| l 372662 | Rattus norvegicus (Norway rat) | Ki | 0.0008 | 1 | 1 |
| l 371257 | Rattus norvegicus (Norway rat) | Ki | 0.0037 | 2 | 2 |
| l 368899 | Rattus norvegicus (Norway rat) | IC50 | 0.3700 | 1 | 1 |
| l 368899 | Rattus norvegicus (Norway rat) | Ki | 0.1100 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| l 701324 | Rattus norvegicus (Norway rat) | Kb | 0.0280 | 1 | 1 |
| mdl 104653 | Rattus norvegicus (Norway rat) | Kb | 0.8800 | 1 | 1 |
Oral oxytocin antagonists.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
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
Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.Journal of medicinal chemistry, , Jul-09, Volume: 36, Issue:14, 1993
Orally active, nonpeptide vasopressin V2 receptor antagonists: a novel series of 1-[4-(benzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepines and related compounds.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
New analgesic drugs derived from phencyclidine.Journal of medicinal chemistry, , Volume: 24, Issue:5, 1981
Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 13, Issue:13, 2003
The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.Bioorganic & medicinal chemistry letters, , Apr-17, Volume: 10, Issue:8, 2000
5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
New, potent, selective, and short-acting peptidic V1a receptor agonists.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
Enhanced selectivity of oxytocin antagonists containing sarcosine in position 7.Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
Preparation and biological activities of potential vasopressin photoaffinity labels.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Oral oxytocin antagonists.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
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
Carbon-11 N-methyl alkylation of L-368,899 and in vivo PET imaging investigations for neural oxytocin receptors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Oral oxytocin antagonists.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010