The Experts below are selected from a list of 3501 Experts worldwide ranked by ideXlab platform
Scott P Runyon - One of the best experts on this subject based on the ideXlab platform.
-
identification of n 6 chloro 4 2 6 dimethoxyphenyl quinazolin 2 yl carbonyl l leucine ntrc 808 a novel nonpeptide chemotype selective for the neurotensin receptor type 2
Bioorganic & Medicinal Chemistry Letters, 2015Co-Authors: James B Thomas, Philippe Sarret, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Danni L Harris, Sanju Narayanan, Scott P RunyonAbstract:Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on known NT receptor nonpeptide compounds, we screened commercial databases to identify compounds that might possess activity at NTS2 receptor sites. Modification of our screening hit to include structural features known to be recognized by NTS1 and NTS2, led to the identification of the novel NTS2 selective nonpeptide, N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (9). This compound is a potent partial agonist in the FLIPR assay with a profile of activity similar to that of the reference NTS2 analgesic nonpeptide levocabastine (5).
-
Identification of 1‑({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)‑1H‑pyrazol-3-yl]carbonyl}amino)cyclohexane Carboxylic Acid as a Selective Nonpeptide Neurotensin Receptor Type 2 Compound
2015Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Angela M. Giddings, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a
-
identification of n 5 4 methylphenyl sulfonyl amino 3 trifluoroacetyl 1h indol 1 yl acetyl l leucine ntrc 824 a neurotensin like nonpeptide compound selective for the neurotensin receptor type 2
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay.
-
identification of 1 1 4 fluorophenyl 5 2 methoxyphenyl 1h pyrazol 3 yl carbonyl amino cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a.
James B Thomas - One of the best experts on this subject based on the ideXlab platform.
-
identification of n 6 chloro 4 2 6 dimethoxyphenyl quinazolin 2 yl carbonyl l leucine ntrc 808 a novel nonpeptide chemotype selective for the neurotensin receptor type 2
Bioorganic & Medicinal Chemistry Letters, 2015Co-Authors: James B Thomas, Philippe Sarret, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Danni L Harris, Sanju Narayanan, Scott P RunyonAbstract:Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on known NT receptor nonpeptide compounds, we screened commercial databases to identify compounds that might possess activity at NTS2 receptor sites. Modification of our screening hit to include structural features known to be recognized by NTS1 and NTS2, led to the identification of the novel NTS2 selective nonpeptide, N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (9). This compound is a potent partial agonist in the FLIPR assay with a profile of activity similar to that of the reference NTS2 analgesic nonpeptide levocabastine (5).
-
Identification of 1‑({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)‑1H‑pyrazol-3-yl]carbonyl}amino)cyclohexane Carboxylic Acid as a Selective Nonpeptide Neurotensin Receptor Type 2 Compound
2015Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Angela M. Giddings, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a
-
identification of n 5 4 methylphenyl sulfonyl amino 3 trifluoroacetyl 1h indol 1 yl acetyl l leucine ntrc 824 a neurotensin like nonpeptide compound selective for the neurotensin receptor type 2
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay.
-
identification of 1 1 4 fluorophenyl 5 2 methoxyphenyl 1h pyrazol 3 yl carbonyl amino cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a.
Jeanmichel Longpre - One of the best experts on this subject based on the ideXlab platform.
-
identification of n 6 chloro 4 2 6 dimethoxyphenyl quinazolin 2 yl carbonyl l leucine ntrc 808 a novel nonpeptide chemotype selective for the neurotensin receptor type 2
Bioorganic & Medicinal Chemistry Letters, 2015Co-Authors: James B Thomas, Philippe Sarret, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Danni L Harris, Sanju Narayanan, Scott P RunyonAbstract:Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on known NT receptor nonpeptide compounds, we screened commercial databases to identify compounds that might possess activity at NTS2 receptor sites. Modification of our screening hit to include structural features known to be recognized by NTS1 and NTS2, led to the identification of the novel NTS2 selective nonpeptide, N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (9). This compound is a potent partial agonist in the FLIPR assay with a profile of activity similar to that of the reference NTS2 analgesic nonpeptide levocabastine (5).
-
Identification of 1‑({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)‑1H‑pyrazol-3-yl]carbonyl}amino)cyclohexane Carboxylic Acid as a Selective Nonpeptide Neurotensin Receptor Type 2 Compound
2015Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Angela M. Giddings, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a
-
identification of n 5 4 methylphenyl sulfonyl amino 3 trifluoroacetyl 1h indol 1 yl acetyl l leucine ntrc 824 a neurotensin like nonpeptide compound selective for the neurotensin receptor type 2
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay.
-
identification of 1 1 4 fluorophenyl 5 2 methoxyphenyl 1h pyrazol 3 yl carbonyl amino cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a.
Philippe Sarret - One of the best experts on this subject based on the ideXlab platform.
-
identification of n 6 chloro 4 2 6 dimethoxyphenyl quinazolin 2 yl carbonyl l leucine ntrc 808 a novel nonpeptide chemotype selective for the neurotensin receptor type 2
Bioorganic & Medicinal Chemistry Letters, 2015Co-Authors: James B Thomas, Philippe Sarret, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Danni L Harris, Sanju Narayanan, Scott P RunyonAbstract:Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on known NT receptor nonpeptide compounds, we screened commercial databases to identify compounds that might possess activity at NTS2 receptor sites. Modification of our screening hit to include structural features known to be recognized by NTS1 and NTS2, led to the identification of the novel NTS2 selective nonpeptide, N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (9). This compound is a potent partial agonist in the FLIPR assay with a profile of activity similar to that of the reference NTS2 analgesic nonpeptide levocabastine (5).
-
Identification of 1‑({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)‑1H‑pyrazol-3-yl]carbonyl}amino)cyclohexane Carboxylic Acid as a Selective Nonpeptide Neurotensin Receptor Type 2 Compound
2015Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Angela M. Giddings, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a
-
identification of n 5 4 methylphenyl sulfonyl amino 3 trifluoroacetyl 1h indol 1 yl acetyl l leucine ntrc 824 a neurotensin like nonpeptide compound selective for the neurotensin receptor type 2
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay.
-
identification of 1 1 4 fluorophenyl 5 2 methoxyphenyl 1h pyrazol 3 yl carbonyl amino cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a.
Robert W Wiethe - One of the best experts on this subject based on the ideXlab platform.
-
identification of n 6 chloro 4 2 6 dimethoxyphenyl quinazolin 2 yl carbonyl l leucine ntrc 808 a novel nonpeptide chemotype selective for the neurotensin receptor type 2
Bioorganic & Medicinal Chemistry Letters, 2015Co-Authors: James B Thomas, Philippe Sarret, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Danni L Harris, Sanju Narayanan, Scott P RunyonAbstract:Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on known NT receptor nonpeptide compounds, we screened commercial databases to identify compounds that might possess activity at NTS2 receptor sites. Modification of our screening hit to include structural features known to be recognized by NTS1 and NTS2, led to the identification of the novel NTS2 selective nonpeptide, N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (9). This compound is a potent partial agonist in the FLIPR assay with a profile of activity similar to that of the reference NTS2 analgesic nonpeptide levocabastine (5).
-
Identification of 1‑({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)‑1H‑pyrazol-3-yl]carbonyl}amino)cyclohexane Carboxylic Acid as a Selective Nonpeptide Neurotensin Receptor Type 2 Compound
2015Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Angela M. Giddings, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a
-
identification of n 5 4 methylphenyl sulfonyl amino 3 trifluoroacetyl 1h indol 1 yl acetyl l leucine ntrc 824 a neurotensin like nonpeptide compound selective for the neurotensin receptor type 2
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay.
-
identification of 1 1 4 fluorophenyl 5 2 methoxyphenyl 1h pyrazol 3 yl carbonyl amino cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound
Journal of Medicinal Chemistry, 2014Co-Authors: James B Thomas, Philippe Sarret, Louis Gendron, Angela M Giddings, Robert W Wiethe, Srinivas Olepu, Keith R Warner, Jeanmichel Longpre, Yanan Zhang, Scott P RunyonAbstract:Compounds active at neurotensin receptors (NTS1 and NTS2) exert analgesic effects on different types of nociceptive modalities, including thermal, mechanical, and chemical stimuli. The NTS2 preferring peptide JMV-431 (2) and the NTS2 selective nonpeptide compound levocabastine (6) have been shown to be effective in relieving the pain associated with peripheral neuropathies. With the aim of identifying novel nonpeptide compounds selective for NTS2, we examined analogues of SR48692 (5a) using a FLIPR calcium assay in CHO cells stably expressing rat NTS2. This led to the discovery of the NTS2 selective nonpeptide compound 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid (NTRC-739, 7b) starting from the nonselective compound 5a.