N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide: a vanilloid receptor 1 antagonist and analgesic; structure in first source [MeSH]
1-piperazinecarboxamide, 4-(3-chloro-2-pyridinyl)-n-[4-(1,1-dimethylethyl)phenyl]- : no description available [CHeBI]
| ID Source | ID |
|---|---|
| PubMed CID | 9929425 |
| CHEMBL ID | 441472 |
| SCHEMBL ID | 1269620 |
| CHEBI ID | 190962 |
| MeSH ID | M0451932 |
| Synonym |
|---|
| n-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2h)-carboxamide |
| gtpl2460 |
| bctc |
| n-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide |
| bctc cpd |
| 4-(3-chloro-pyridin-2-yl)-piperazine-1-carboxylic acid (4-tert-butyl-phenyl)-amide |
| bdbm50133817 |
| CHEMBL441472 , |
| 1-piperazinecarboxamide, 4-(3-chloro-2-pyridinyl)-n-[4-(1,1-dimethylethyl)phenyl]- |
| CHEBI:190962 |
| 4-(3-chloro-2-pyridinyl)-n-[4-(1,1-dimethylethyl)phenyl]-1-piperazinecarboxamide, bctc |
| mfcd08690556 |
| 393514-24-4 |
| S6838 |
| SCHEMBL1269620 |
| 4-(3-chloro-2-pyridinyl)-n-[4-(1,1-dimethylethyl)phenyl]-1-piperazinecarboxamide |
| HB1190 |
| AKOS024457842 |
| c20h25cln4o |
| DTXSID90432997 |
| FT-0696667 |
| HY-19960 |
| CS-5476 |
| n-(4-t-butylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2h)-carboxamide |
| AS-73732 |
| bctc, >=98% (hplc) |
| NCGC00370959-01 |
| BCP19629 |
| Q27074955 |
| CCG-356434 |
| n-(4-(tert-butyl)phenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide |
| EX-A4527 |
| A912829 |
| BB165272 |
| Class | Description |
|---|---|
| piperazines | |
| pyridines | Any organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives. |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 10.6840 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 6.0081 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 11.9877 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 6.0081 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 6.0081 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 6.0081 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 6.0081 | AID1645842 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Transient receptor potential cation channel subfamily A member 1 | Homo sapiens (human) | EC50 | 4.5000 | AID470071 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560 | 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID763712 | Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of capsaicin-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Design and synthesis of conformationally restricted capsaicin analogues based in the 1, 3, 4-thiadiazole heterocycle reveal a novel family of transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID1177526 | Antagonist activity against human TRPA1 expressed in T-REx HEK cells assessed as inhibition of AITC-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to AITC stimulation by Fluo-4 AM dye based fluorescence assay | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID1066637 | Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of cold-induced intracellular Ca2+ influx by Fluo-8 AM staining-based fluorescence analysis | 2014 | Journal of natural products, Feb-28, Volume: 77, Issue:2 ISSN: 1520-6025 | Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. |
| AID313135 | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID266314 | Antagonist activity against capsaicin-induced 45calcium ion uptake in CHO cells expressing rat TRPV1 | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 ISSN: 0022-2623 | Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles. |
| AID1373244 | Antinociceptive activity in heat-induced pain mouse model assessed as increase in tail-flick latency at 30 mg/kg pretreated for 30 mins followed by acetic acid challenge measured for 12 secs post acetic acid challenge by tail-flick test | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 ISSN: 1464-3391 | Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide. |
| AID1691525 | Analgesic activity in acetic acid-induced rat model of abdominal constriction assessed as reduction in number of writhes at 30 mg/kg, po administered as single dose | 2020 | European journal of medicinal chemistry, May-15, Volume: 194ISSN: 1768-3254 | Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide. |
| AID313144 | Oral bioavailability in rat | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID1177525 | Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to capsaicin stimulation by Fluo-4 AM dye based fluorescence assay | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID1272990 | Analgesic activity in heat-induced KM mouse pain model assessed as delay in tail-filck response at 30 mg/kg, po | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1. |
| AID1177524 | Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of cold-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to cold stimulation by Fluo-4 AM dye based fluorescence assay | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID1691519 | Induction of hyperthermia in rat assessed as change in body temperature at 30 mg/kg, po administered as single dose measured after 30 to 60 mins by rectal thermometric method | 2020 | European journal of medicinal chemistry, May-15, Volume: 194ISSN: 1768-3254 | Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide. |
| AID1691526 | Analgesic activity in rat assessed as increase in tail flick latency at 30 mg/kg, po administered as single dose by tail-flick test | 2020 | European journal of medicinal chemistry, May-15, Volume: 194ISSN: 1768-3254 | Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide. |
| AID763714 | Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of capsaicin-induced calcium flux at 1 uM after 30 mins by Fluo-4AM based fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Design and synthesis of conformationally restricted capsaicin analogues based in the 1, 3, 4-thiadiazole heterocycle reveal a novel family of transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID1177519 | Agonist activity at human TRPV1 expressed in T-REx HEK cells assessed as increase in intracellular Ca2+ accumulation by Fluo-4 AM dye based fluorescence assay relative to ionomycin | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID763715 | Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of temperature-induced calcium flux at 1 uM after 30 mins by Fluo-4AM based fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Design and synthesis of conformationally restricted capsaicin analogues based in the 1, 3, 4-thiadiazole heterocycle reveal a novel family of transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID313139 | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID266315 | Antagonist activity against acid-induced 45calcium ion uptake in CHO cells expressing rat TRPV1 at pH5 | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 ISSN: 0022-2623 | Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles. |
| AID1373241 | Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced intracellular calcium level preincubated for 2.5 mins followed by capsaicin addition measured for 5 mins by aequorin dye based assay | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 ISSN: 1464-3391 | Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide. |
| AID1066642 | Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of icilin-induced intracellular Ca2+ influx at 0.3 to 10 uM by fluorescence-based assay | 2014 | Journal of natural products, Feb-28, Volume: 77, Issue:2 ISSN: 1520-6025 | Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. |
| AID1289986 | Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol mediated current amplitude at +80 mV holding potential by whole cell patch-clamp assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 ISSN: 1520-4804 | Tryptamine-Based Derivatives as Transient Receptor Potential Melastatin Type 8 (TRPM8) Channel Modulators. |
| AID1691523 | Antagonist activity at human TRPV1 assessed as inhibition of pH 5-induced channel activation at 10 uM relative to control | 2020 | European journal of medicinal chemistry, May-15, Volume: 194ISSN: 1768-3254 | Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide. |
| AID10772 | Plasma clearance in rat by iv administration at a dose of 3 mg/kg | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| AID1451859 | Displacement of [3H]RTX from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting method | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19 ISSN: 1520-4804 | Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1). |
| AID1177518 | Agonist activity at human TRPV1 expressed in T-REx HEK cells assessed as increase in intracellular Ca2+ accumulation by Fluo-4 AM dye based fluorescence assay | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID1177516 | Agonist activity at mouse TRPM8 expressed in T-REx HEK cells assessed as increase in intracellular Ca2+ accumulation by Fluo-4 AM dye based fluorescence assay | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID1272989 | Analgesic activity in proton-induced KM mouse pain model assessed as suppression of acetic acid-induced writhing response at 30 mg/kg, po dosed 30 mins before acetic acid challenge | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1. |
| AID1567462 | Antagonist activity at capsaicin-induced human recombinant TRPV1 expressed in CHO-K1 cells co-expressing aequorin incubated for 2.5 mins in presence of ATP followed by capsaicin addition by luminescence assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID1410815 | Antagonist activity at TRPM8 (unknown origin) assessed as reduction in menthol-induced calcium influx | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 ISSN: 1520-4804 | Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. |
| AID1567482 | Antinociceptive activity in KM mouse model of acetic acid induced pain assessed as suppression of writhes at 1 to 10 mg/kg, po administered as single dose pretreated for 30 mins followed by acetic acid challenge and measured for 15 mins | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID1066628 | Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of proton-induced intracellular Ca2+ influx at 10 uM by fluorescence-based assay | 2014 | Journal of natural products, Feb-28, Volume: 77, Issue:2 ISSN: 1520-6025 | Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. |
| AID1177523 | Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of icilin-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to icilin stimulation by Fluo-4 AM dye based fluorescence assay | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID1272988 | Analgesic activity in capsaicin-induced KM mouse assessed as reduction in paw licking time at 30 mg/kg, po dosed 30 mins before capsaicin challenge | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1. |
| AID1066645 | Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of menthol-induced intracellular Ca2+ influx by fluorescence-based assay | 2014 | Journal of natural products, Feb-28, Volume: 77, Issue:2 ISSN: 1520-6025 | Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. |
| AID10896 | Tmax in rat by po administration at a dose of 40 mg/kg | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| AID1567483 | Antinociceptive activity in KM mouse model of thermal-induced nociception assessed as increase in latency to tail withdrawal at 1 to 10 mg/kg, po administered as single dose pretreated for 30 mins | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID1567461 | Effect on body temperature in KM mouse assessed as increase in rectal temperature at 10 mg/kg, po administered as single dose measured every 30 mins for 120 mins by electric probe thermometer | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID237660 | In vivo clearance of compound after intravenous administration in rats at concentration of 3 mg/kg was determined | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 ISSN: 0960-894X | Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists. |
| AID1177521 | Agonist activity at human TRPA1 expressed in T-REx HEK cells assessed as increase in intracellular Ca2+ accumulation by Fluo-4 AM dye based fluorescence assay relative to ionomycin | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID1373243 | Antinociceptive activity in proton-induced pain mouse model assessed as reduction in acetic acid-induced writhes at 30 mg/kg pretreated for 30 mins followed by acetic acid challenge measured for 15 mins post acetic acid challenge | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 ISSN: 1464-3391 | Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide. |
| AID1066646 | Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay | 2014 | Journal of natural products, Feb-28, Volume: 77, Issue:2 ISSN: 1520-6025 | Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. |
| AID763713 | Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of temperature-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Design and synthesis of conformationally restricted capsaicin analogues based in the 1, 3, 4-thiadiazole heterocycle reveal a novel family of transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID387155 | Analgesic activity against complete Freund's adjuvant-induced thermal hyperalgesia in po dosed Sprague-Dawley rat assessed as paw withdrawal latency | 2008 | Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18 ISSN: 1464-3391 | Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID1066654 | Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of heat-induced intracellular Ca2+ influx measured for 42 mins by fluorescence-based assay | 2014 | Journal of natural products, Feb-28, Volume: 77, Issue:2 ISSN: 1520-6025 | Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. |
| AID1744410 | Antagonist activity at human TRPV1 expressed in HEK cells assessed as inhibition of 10 nM capsaicin-induced calcium uptake by FLIPR assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 ISSN: 1520-4804 | Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift. |
| AID1177520 | Agonist activity at human TRPA1 expressed in T-REx HEK cells assessed as increase in intracellular Ca2+ accumulation by Fluo-4 AM dye based fluorescence assay | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID470071 | Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as decrease in intracellular calcium level | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 ISSN: 1464-3405 | Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands. |
| AID11490 | Pharmacokinetic (PK) parameter Vz in rat | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| AID1875056 | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular calcium accumulation preincubated with compound followed by capsaicin addition and measured at 180 sec by fluorescence based microplate | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 ISSN: 1520-4804 | |
| AID1373242 | Aqueous solubility of the compound | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 ISSN: 1464-3391 | Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide. |
| AID1177522 | Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of menthol-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to menthol stimulation by Fluo-4 AM dye based fluorescence assay | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID313138 | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID1272992 | Toxicity in KM mouse assessed as hyperthermia at 30 mg/kg, ig measured from 30 to 90 mins by electric probe thermometric analysis relative to vehicle-treated control | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1. |
| AID387156 | Antinociceptive activity against hyperalgesia in po dosed rat Chung neuropathic pain model | 2008 | Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18 ISSN: 1464-3391 | Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID1567463 | Antagonist activity at low pH-induced human recombinant TRPV1 expressed in CHO-K1 cells co-expressing aequorin at 50 uM incubated for 2.5 mins in presence of ATP followed by hydrochloride addition at pH 5 by luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID1066653 | Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of proton-induced intracellular Ca2+ influx at 100 uM by fluorescence-based assay | 2014 | Journal of natural products, Feb-28, Volume: 77, Issue:2 ISSN: 1520-6025 | Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. |
| AID470068 | Inhibition of FAAH-mediated hydrolysis of [3H]AEA in rat brain membrane | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 ISSN: 1464-3405 | Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands. |
| AID1498465 | Displacement of [3H]RTX from human TRPV1 expressed in HEK293 cell membranes after 60 mins by scintillation counting method | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 ISSN: 1464-3391 | Design, synthesis, and biological evaluation of novel biphenyl-4-carboxamide derivatives as orally available TRPV1 antagonists. |
| AID218485 | Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| AID242493 | Inhibition of human vanilloid receptor 1 in HEK293 cells in capsaicin-induced FLIPR assay | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 ISSN: 0960-894X | Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists. |
| AID1392653 | Toxicity in C57BL/6 mouse assessed as change in body temperature at 3 mg/kg, iv after 120 mins | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 ISSN: 1520-4804 | Targeting Transient Receptor Potential Vanilloid 1 (TRPV1) Channel Softly: The Discovery of Passerini Adducts as a Topical Treatment for Inflammatory Skin Disorders. |
| AID763711 | Antagonist activity at chicken TRPV1 receptor assessed as inhibition of capsaicin-induced calcium flux at 1 uM after 30 mins by cell based Fluo-4AM fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Design and synthesis of conformationally restricted capsaicin analogues based in the 1, 3, 4-thiadiazole heterocycle reveal a novel family of transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID1875055 | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular calcium accumulation at 100 nM preincubated with compound followed by capsaicin addition and measured at 180 sec by fluorescence based m | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 ISSN: 1520-4804 | |
| AID1289989 | Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol mediated current amplitude at 3 uM at +80 mV holding potential measured after drug wash out by whole cell patch-clamp assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 ISSN: 1520-4804 | Tryptamine-Based Derivatives as Transient Receptor Potential Melastatin Type 8 (TRPM8) Channel Modulators. |
| AID218460 | Antagonistic activity against vanilloid receptor 1 (TRPV1) | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11 ISSN: 0022-2623 | Vanilloid receptor TRPV1 antagonists as the next generation of painkillers. Are we putting the cart before the horse? |
| AID1066644 | Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of icilin-induced intracellular Ca2+ influx by fluorescence-based assay | 2014 | Journal of natural products, Feb-28, Volume: 77, Issue:2 ISSN: 1520-6025 | Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. |
| AID1451870 | Displacement of [3H]MPOU from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting method | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19 ISSN: 1520-4804 | Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1). |
| AID237303 | In vivo half life of compound after intravenous administration in rats at concentration of 3 mg/kg was determined | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 ISSN: 0960-894X | Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists. |
| AID237952 | Rat liver metabolic stability was determined | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 ISSN: 0960-894X | Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists. |
| AID1567481 | Antinociceptive activity in KM mouse model of capsaicin-induced pain assessed as reduction in paw licking time at 1 to 10 mg/kg, po administered as single dose pretreated for 30 mins followed by capsaicin challenge and measured for 5 mins | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID1177517 | Agonist activity at mouse TRPM8 expressed in T-REx HEK cells assessed as increase in intracellular Ca2+ accumulation by Fluo-4 AM dye based fluorescence assay relative to ionomycin | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 ISSN: 1520-6025 | Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives. |
| AID779486 | Inhibition of TRPM8 (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 ISSN: 1464-3391 | Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists. |
| AID237790 | In vivo volume of distribution of compound after intravenous administration in rats at concentration of 3 mg/kg was determined | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 ISSN: 0960-894X | Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists. |
| AID313137 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID1567475 | Antinociceptive activity in KM mouse model of acetic acid induced pain assessed as suppression of writhes at 30 mg/kg, po administered as single dose pretreated for 30 mins followed by acetic acid challenge and measured for 15 mins | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID470069 | Inhibition of FAAH-mediated hydrolysis of [3H]AEA in rat brain membrane at 50 uM | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 ISSN: 1464-3405 | Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands. |
| AID1272985 | Antagonist activity at capsaicin-stimulated human TRPV1 receptor in aequorin expressing cells preincubated for 2.5 mins followed by capsaicin addition | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1. |
| AID1481479 | Antagonist activity at recombinant human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced activation | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 ISSN: 1464-3391 | Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain. |
| AID313134 | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID779485 | Inhibition of TRPV1 (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 ISSN: 1464-3391 | Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists. |
| AID313141 | Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID387154 | Ratio of drug level in brain to plasma in po dosed Sprague-Dawley rat | 2008 | Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18 ISSN: 1464-3391 | Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID236064 | Bioavailability in rat (single dose 30 mg/kg p.o.) | 2005 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3 ISSN: 0960-894X | 4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists. |
| AID1272987 | Inhibition of ovine COX1 at 10 uM by enzyme immunoassay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1. |
| AID1567479 | Effect on body temperature in KM mouse assessed as increase in rectal temperature at 30 mg/kg, po administered as single dose measured every 30 mins for 90 mins by electric probe thermometer | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID1875053 | Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium accumulation by measuring efficacy at 100 nM measured at 180 sec by fluorescence based microplate reader analysis relative to capsaicin | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 ISSN: 1520-4804 | |
| AID313136 | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID1399075 | Aqueous solubility of the compound incubated for 72 hrs under shaking condition by HPLC method | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 ISSN: 1464-3391 | Novel benzodiazepines derivatives as analgesic modulating for Transient receptor potential vanilloid 1. |
| AID1495475 | Antinociceptive activity in Kunming mouse model of thermal-induced nociception assessed as increase in latency to tail withdrawal at 60 mg/kg, po by tail flick test | 2018 | Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel hydrogen sulfide releasing capsaicin derivatives. |
| AID12648 | Half life period in rat by iv administration at a dose of 3 mg/kg | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| AID11432 | Cmax in rat by po administration at a dose of 40 mg/kg | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| AID1567476 | Antinociceptive activity in KM mouse model of thermal-induced nociception assessed as increase in latency to tail withdrawal at 30 mg/kg, po administered as single dose pretreated for 30 mins | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID1399071 | Inhibition of human TRPV1 expressed in HEK293 cells assessed as reduction in capsaicin-induced activity pretreated for 2.5 mins followed by capsaicin addition measured immediately in presence of coelenterazine h | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15 ISSN: 1464-3391 | Novel benzodiazepines derivatives as analgesic modulating for Transient receptor potential vanilloid 1. |
| AID1691522 | Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced channel activation | 2020 | European journal of medicinal chemistry, May-15, Volume: 194ISSN: 1768-3254 | Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide. |
| AID242439 | Inhibition of human vanilloid receptor 1 in HEK293 cells in pH 5.5-induced FLIPR assay | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 ISSN: 0960-894X | Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists. |
| AID1567474 | Antinociceptive activity in KM mouse model of capsaicin-induced pain assessed as reduction in paw licking time at 30 mg/kg, po administered as single dose pretreated for 30 mins followed by capsaicin challenge and measured for 5 mins | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. |
| AID1272986 | Inhibition of human recombinant COX2 at 10 uM by enzyme immunoassay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1. |
| AID13439 | Oral bioavailability in rat by po administration at a dose of 40 mg/kg | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 ISSN: 1768-3254 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
| AID1481466 | Antagonist activity at recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins followed by 4alphaPDD stimulation measured for 5 mins by FLIPR assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 ISSN: 1464-3391 | Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain. |
| AID218486 | Vanilloid receptor subtype 1 antagonist activity based on its ability to block low pH-induced activation of the rat VR1 channel in a HEK293 cell line | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| AID1875052 | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced intracellular calcium accumulation at 10 uM preincubated with compound followed by capsaicin addition and measured at 180 sec by fluorescence based mi | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 ISSN: 1520-4804 | |
| AID313140 | Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 ISSN: 0022-2623 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. |
| AID1691524 | Analgesic activity in capsaicin-induced rat model of hyperalgesia assessed as reduction in total paw licking time at 30 mg/kg, po administered as single dose | 2020 | European journal of medicinal chemistry, May-15, Volume: 194ISSN: 1768-3254 | Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide. |
| AID1289988 | Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol mediated current amplitude at 3 uM at +80 mV holding potential by whole cell patch-clamp assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 ISSN: 1520-4804 | Tryptamine-Based Derivatives as Transient Receptor Potential Melastatin Type 8 (TRPM8) Channel Modulators. |
| AID470070 | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as decrease in intracellular calcium level | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 ISSN: 1464-3405 | Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands. |
| AID387153 | Antagonist activity at human recombinant TRPV1 expressed in human 1321N1 cells assessed as inhibition of capsaicin-induced calcium influx by FLIPR assay | 2008 | Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18 ISSN: 1464-3391 | Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. |
| AID244059 | Percent inhibition of human ether-a-go-go related gene (hERG) channel expressed in HEK293 cells in standard whole cell voltage-clamp assay | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 ISSN: 0960-894X | Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists. |
| AID1346617 | Human TRPV1 (Transient Receptor Potential channels) | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 ISSN: 1464-3391 | Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists. |
| AID1346643 | Rat TRPV1 (Transient Receptor Potential channels) | 2003 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 306, Issue:1 ISSN: 0022-3565 | N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties. |
| AID493017 | Wombat Data for BeliefDocking | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 ISSN: 0960-894X | 4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 28 (34.15) | 29.6817 |
| 2010's | 49 (59.76) | 24.3611 |
| 2020's | 5 (6.10) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (1.20%) | 5.53% |
| Reviews | 2 (2.41%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 80 (96.39%) | 84.16% |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Ache | 0 | 2003 | 2018 | 13.3 | low | 1 | 0 | 0 | 6 | 4 | 0 | |
| Acidosis | 0 | 2017 | 2017 | 7.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Allodynia | 0 | 2003 | 2018 | 13.6 | low | 0 | 0 | 0 | 5 | 4 | 0 | |
| Alloxan Diabetes | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Ataxia | 0 | 2003 | 2003 | 21.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Benign Neoplasms | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Bladder, Overactive | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Blood Poisoning | 0 | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Bowel Diseases, Inflammatory | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cancer of Prostate | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cardiac Failure | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cardiac Hypertrophy | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cardiomegaly | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Chronic Disease | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Chronic Illness | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Colitis | 0 | 2006 | 2014 | 13.8 | low | 0 | 0 | 0 | 2 | 2 | 0 | |
| Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Constriction, Pathologic | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Constriction, Pathological | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Dermatoses | 0 | 2010 | 2018 | 10.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Disease Models, Animal | 0 | 2006 | 2020 | 12.1 | medium | 0 | 0 | 0 | 5 | 8 | 0 | |
| Dry Eye | 0 | 2010 | 2012 | 13.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Dry Eye Syndromes | 0 | 2010 | 2012 | 13.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Fever | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Gastric Stasis | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Gastroparesis | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Heart Failure | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Hyperplasia | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Ileus | 0 | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Inflammation | 0 | 2003 | 2018 | 13.5 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Inflammatory Bowel Diseases | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Injuries, Spinal Cord | 0 | 2005 | 2005 | 19.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Innate Inflammatory Response | 0 | 2003 | 2018 | 13.5 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Metabolic Acidosis | 0 | 2017 | 2017 | 7.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Muscle Contraction | 0 | 2009 | 2015 | 12.0 | low | 0 | 0 | 0 | 1 | 2 | 0 | |
| Muscle Relaxation | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Necrosis | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Neoplasms | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Nerve Pain | 0 | 2013 | 2018 | 8.5 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
| Nervous System Diseases | 0 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Nervous System Disorders | 0 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Neuralgia | 0 | 2013 | 2018 | 8.5 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
| Pain | 0 | 2003 | 2018 | 13.3 | low | 1 | 0 | 0 | 6 | 4 | 0 | |
| Peripheral Nerve Diseases | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Peripheral Nervous System Diseases | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Prostatic Neoplasms | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Pyrexia | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Sepsis | 0 | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Skin Diseases | 0 | 2010 | 2018 | 10.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Spinal Cord Injuries | 0 | 2005 | 2005 | 19.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Urinary Bladder, Overactive | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Article | Year |
|---|---|
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5 | 2019 |
| Design, synthesis and biological evaluation of novel hydrogen sulfide releasing capsaicin derivatives. Bioorganic & medicinal chemistry, , 05-15, Volume: 26, Issue:9 | 2018 |
| Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles. Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12 | 2006 |
| N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties. The Journal of pharmacology and experimental therapeutics, , Volume: 306, Issue:1 | 2003 |
| Article | Year |
|---|---|
| Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists. Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21 | 2013 |
| Pharmacologic antagonism of the oral aversive taste-directed response to capsaicin in a mouse brief access taste aversion assay. The Journal of pharmacology and experimental therapeutics, , Volume: 332, Issue:2 | 2010 |
| Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18 | 2008 |