| Assay ID | Title | Year | Journal | Article |
|---|
| AID578505 | Displacement of [3H]AVP from human vasopressin V1a receptor at 5 uM | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. |
| AID598597 | Volume of distribution at steady state in rat at 2 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID481295 | Biodistribution in baboon liver at 2.5+/-0.8 mCi, iv followed by second dose administered > 2 hrs after initial dose measured per cc after 90 mins | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography. |
| AID598592 | Intrinsic clearance in rat liver microsomes measured up to 40 mins by HPLC-MS method | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID598600 | Ratio of AUC in brain to plasma in rat at 10 mg/kg, ip | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID481301 | Selectivity ratio of vasopressin V1b receptor over vasopressin V2 receptor | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography. |
| AID598587 | Displacement of [3H]AVP from human vasopressin V1b receptor expressed in CHO cells by scintillation counting | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID598596 | Terminal half life in rat at 2 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID578504 | Displacement of [3H]AVP from rat vasopressin V1b receptor expressed in CHO cells by whole cell binding assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. |
| AID578503 | Displacement of [3H]AVP from human vasopressin V1b receptor expressed in CHO cells by whole cell binding assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. |
| AID598588 | Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cells by scintillation counting | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID552047 | Antagonist activity at recombinant V1a receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| The characterization of a novel V1b antagonist lead series. |
| AID439090 | Displacement of [3H]Arg8-vasopressin from rat vasopressin V1b receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
| Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. |
| AID481296 | Biodistribution in baboon heart at 2.5+/-0.8 mCi, iv followed by second dose administered > 2 hrs after initial dose measured per cc after 90 mins | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography. |
| AID552048 | Antagonist activity at recombinant oxytocin receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| The characterization of a novel V1b antagonist lead series. |
| AID598598 | Clearance in rat plasma at 2 mg/kg, iv | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID481302 | Selectivity ratio of vasopressin V1b receptor over oxytocin receptor | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography. |
| AID439091 | Displacement of [3H]Arg8-vasopressin from human vasopressin V1a receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
| Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. |
| AID439089 | Displacement of [3H]Arg8-vasopressin from human vasopressin V1b receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
| Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. |
| AID598590 | Displacement of radiolabeled oxytocin from human oxytocin receptor expressed in CHO cells by scintillation counting | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID598591 | Intrinsic clearance in human liver microsomes measured up to 40 mins by HPLC-MS method | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID481297 | Biodistribution in baboon spleen at 2.5+/-0.8 mCi, iv followed by second dose administered > 2 hrs after initial dose measured per cc after 90 mins | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography. |
| AID598589 | Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID552046 | Antagonist activity at recombinant V1b receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| The characterization of a novel V1b antagonist lead series. |
| AID578506 | Displacement of [3H]AVP from human vasopressin V2 receptor | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. |
| AID439092 | Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
| Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. |
| AID481300 | Selectivity ratio of vasopressin V1b receptor over vasopressin V1a receptor | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography. |
| AID481298 | Biodistribution in baboon lung at 2.5+/-0.8 mCi, iv followed by second dose administered > 2 hrs after initial dose measured per cc after 90 mins | 2010 | Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
| Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography. |
| AID439088 | Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
| Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. |
| AID578507 | Displacement of [3H]oxytocin from human oxytocin receptor | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. |
| AID598599 | Oral bioavailability in rat plasma at 10 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. |
| AID1346432 | Human V1A receptor (Vasopressin and oxytocin receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist |
| AID1346469 | Human OT receptor (Vasopressin and oxytocin receptors) | 2005 | British journal of pharmacology, Nov, Volume: 146, Issue:5
| Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. |
| AID1346469 | Human OT receptor (Vasopressin and oxytocin receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist |
| AID1346460 | Human V1B receptor (Vasopressin and oxytocin receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist |
| AID1346460 | Human V1B receptor (Vasopressin and oxytocin receptors) | 2005 | British journal of pharmacology, Nov, Volume: 146, Issue:5
| Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. |
| AID1346453 | Human V2 receptor (Vasopressin and oxytocin receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist |
| AID1346460 | Human V1B receptor (Vasopressin and oxytocin receptors) | 2002 | Proceedings of the National Academy of Sciences of the United States of America, Apr-30, Volume: 99, Issue:9
| Anxiolytic- and antidepressant-like effects of the non-peptide vasopressin V1b receptor antagonist, SSR149415, suggest an innovative approach for the treatment of stress-related disorders. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |