| Assay ID | Title | Year | Journal | Article |
|---|
| AID1220136 | Tmax in male beagle dog plasma at 10 mg/kg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID1220198 | Half life in male beagle dog plasma at 10 mg/kg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID217376 | In vitro binding affinity to human V2 receptor | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
| 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. |
| AID213782 | In vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membrane | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
| 4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists. |
| AID217389 | Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells. | 2003 | Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
| Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists. |
| AID1220194 | AUC(0 to t) in female Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID181602 | Antagonistic effect against Vasopressin V2 at 1 mg/kg dosed (ip) into rat with 0.4 ug/kg of AVP (in peanut oil); negative | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID181608 | Antagonistic effect against Vasopressin V2 at 10 mg/kg dosed (ip) into rat with 0.4 ug/kg of AVP (in peanut oil); negative | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID217839 | Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes. | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID217555 | Binding affinity to rat V2 receptor | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
| 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. |
| AID181604 | Antagonistic effect against Vasopressin V2 at 10 mg/kg administered orally (by gavage) 30 mL/kg of deionized water in second experiment; positive | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID1220131 | Tmax in female Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID188451 | Urinary osmolality from urine collected from rat at 3 mg/kg | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID310569 | Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies. |
| AID301764 | Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
| Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. |
| AID181601 | Antagonistic effect against Vasopressin V2 at 1 mg/kg dosed (ip) into rat with 0.4 ug/kg of AVP (in peanut oil) in second experiment | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID217527 | Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
| Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity. |
| AID1220193 | Half life in female Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID13270 | Amount of urine output was measured in rat at a dose of 10 mg/kg administered orally | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
| 4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists. |
| AID1220188 | Half life in male Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID301768 | Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
| Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. |
| AID1220192 | Cmax in female Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID191003 | Urine volume collected after 10 mg/kg of drug administration into 6 rats. | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID188447 | Urinary osmolality from urine collected from rat at 1 mg/kg | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID191009 | Aquaretic effect was measured by the amount of urine collected after 4 hr at a dose of 10 mg/kg ip in 2 Dawley rats | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
| Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists. |
| AID1220201 | Cmax in human plasma at 100 mg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID217212 | Inhibition of 1 nM AVP-induced calcium mobilisation in cells expressing human vasopressin V1a receptor | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
| Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates. |
| AID217378 | Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
| The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery. |
| AID181610 | Antagonistic effect against Vasopressin V2 at 3 mg/kg administered orally (by gavage) 30 mL/kg of deionized water in second experiment; positive | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID1220137 | Cmax in male beagle dog plasma at 10 mg/kg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID217682 | Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor. | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
| Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists. |
| AID1220184 | AUC(0 to t) in human plasma at 100 mg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID254873 | Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| (4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators. |
| AID217072 | Binding affinity towards human V1a receptors | 2003 | Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
| Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists. |
| AID1220121 | Tmax in human plasma at 100 mg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID1220200 | AUC(0 to infinity) in male beagle dog plasma at 10 mg/kg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID1220199 | AUC(0 to t) in male beagle dog plasma at 10 mg/kg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID217845 | Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID216933 | Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
| Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates. |
| AID217080 | Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
| Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity. |
| AID256436 | Urine volume in AVP treated rat at 0.4 ug/kg upon oral administration during 4 hr was determined | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| (4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators. |
| AID213933 | Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
| 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. |
| AID181611 | Antagonistic effect against Vasopressin V2 at 3 mg/kg administered orally (by gavage) 30 mL/kg of deionized water; negative | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID217075 | In vitro binding affinity to human V1a receptor | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
| 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. |
| AID181607 | Antagonistic effect against Vasopressin V2 at 10 mg/kg dosed (ip) into rat with 0.4 ug/kg of AVP (in peanut oil) in second experiment; positive | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID188452 | Urinary osmolality from urine collected from rat at 3 mg/kg in second experiment | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID1220183 | Half life in human plasma at 100 mg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID1220115 | AUC at steady state in human at 100 mg, po qd for 7 days by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID181613 | Antagonistic effect against Vasopressin V2 at 3 mg/kg dosed (ip) into rat with 0.4 ug/kg of AVP (in peanut oil) in second experiment; positive | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID217846 | Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla. | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID191500 | Urine volume was measured after 4 hours following oral compound dose of 3 mg/kg in rats deprived with food or water | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
| 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. |
| AID217840 | Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes. | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID1220125 | AUC(0 to infinity) in human plasma at 100 mg, po administered as single dose by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID216934 | Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
| Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates. |
| AID188450 | Urinary osmolality from urine collected from rat at 10 mg/kg in second experiment | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID301770 | Effect on urine volume in rat 10 mg/kg, po relative to control | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
| Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. |
| AID217224 | In vitro binding affinity for rat V1a receptor | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
| 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. |
| AID255037 | Inhibition of [3H]-AVP binding to human V2 receptor | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| (4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators. |
| AID191005 | Urine volume collected after 1 mg/kg of drug administration into 6 rats | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID217209 | Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
| Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity. |
| AID217213 | Inhibition of [3H]AVP binding to recombinant human vasopressin V1a receptor | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
| Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates. |
| AID181598 | Antagonistic effect against Vasopressin V2 at 1 mg/kg administered orally (by gavage) 30 mL/kg of deionized water in second experiment; positive | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID310566 | Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies. |
| AID187252 | Ratio of rat urine volume collected from treatment group (10 mg/kg perorally) after 4 hours versus control group was determined | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
| The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery. |
| AID310564 | Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies. |
| AID1220135 | AUC(0 to infinity) in female Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID188449 | Urinary osmolality from urine collected from rat at 10 mg/kg | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID191008 | Urine volume collected after 3 mg/kg of drug administration into 15 rats | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID1220186 | Tmax in male Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID191006 | Urine volume collected after 1 mg/kg of drug administration into 8 rats. (Conscious rats free access to water before but not during the experiment). | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID301767 | Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
| Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. |
| AID1220129 | AUC(0 to t) in male Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID1220127 | Cmax in male Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID190999 | Urine volume collected after 10 mg/kg of drug administration into 13 rats. (Conscious rats free access to water before and after during the experiment) | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID181599 | Antagonistic effect against Vasopressin V2 at 1 mg/kg administered orally (by gavage) 30 mL/kg of deionized water; negative | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID1220190 | AUC(0 to infinity) in male Sprague-Dawley rat plasma at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID181605 | Antagonistic effect against Vasopressin V2 at 10 mg/kg administered orally (by gavage) 30 mL/kg of deionized water; negative | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID181614 | Antagonistic effect against Vasopressin V2 at 3 mg/kg dosed (ip) into rat with 0.4 ug/kg of AVP (in peanut oil); negative | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID310568 | Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies. |
| AID188448 | Urinary osmolality from urine collected from rat at 1 mg/kg in second experiment | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID10910 | Amount of urine output was measured in rat at a dose of 10 mg/kg/po | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
| 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. |
| AID191499 | Urine volume was measured after 4 hours following oral compound dose of 10 mg/kg in a volume of 10 mL/kg (20% dimethylsulfoxide in 2.5% preboiled starch) in rats deprived with food or water | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
| 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. |
| AID191007 | Urine volume collected after 3 mg/kg of drug administration into 10 rat | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID234932 | Relative affinity for human vasopressin receptors V1a and V2 | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID213785 | Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
| 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. |
| AID234937 | Relative affinity for rat vasopressin receptors V1a and V2 | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| AID217386 | Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
| Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity. |
| AID213916 | In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2) | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13
| 4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists. |
| AID217228 | Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor. | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
| Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists. |
| AID1220114 | Drug concentration at steady state in human at 100 mg, po qd for 7 days by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346453 | Human V2 receptor (Vasopressin and oxytocin receptors) | 2000 | Kidney international, Oct, Volume: 58, Issue:4
| Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463. |
| AID1346453 | Human V2 receptor (Vasopressin and oxytocin receptors) | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |