Page last updated: 2024-08-07 16:17:22
Substance-P receptor
A substance-P receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P25103]
Synonyms
SPR;
NK-1 receptor;
NK-1R;
Tachykinin receptor 1
Research
Bioassay Publications (88)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 30 (34.09) | 18.2507 |
| 2000's | 33 (37.50) | 29.6817 |
| 2010's | 24 (27.27) | 24.3611 |
| 2020's | 1 (1.14) | 2.80 |
Compounds (52)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| sb 223412 | Homo sapiens (human) | Kb | 0.0030 | 1 | 1 |
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Non-peptide NK1 receptor ligands based on the 4-phenylpyridine moiety.Bioorganic & medicinal chemistry, , Apr-01, Volume: 19, Issue:7, 2011
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Design, synthesis, and structure-affinity relationship studies in NK1 receptor ligands based on azole-fused quinolinecarboxamide moieties.Bioorganic & medicinal chemistry, , Jul-15, Volume: 16, Issue:14, 2008
A non-peptide NK1 receptor agonist showing subpicomolar affinity.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Solution structures in SDS micelles and functional activity at the bullfrog substance P receptor of ranatachykinin peptides.Journal of medicinal chemistry, , May-04, Volume: 43, Issue:9, 2000
Asymmetric synthesis of Boc-N-methyl-p-benzoyl-phenylalanine. Preparation of a photoreactive antagonist of substance P.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 8, Issue:11, 1998
Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.Bioorganic & medicinal chemistry letters, , Feb-03, Volume: 8, Issue:3, 1998
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Synthesis, modelling and NK1 antagonist evaluation of a non-rigid cyclopropane-containing analogue of CP-99,994.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
Aza-tricyclic substance P antagonists.Journal of medicinal chemistry, , Sep-02, Volume: 37, Issue:18, 1994
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.Journal of medicinal chemistry, , Apr-29, Volume: 37, Issue:9, 1994
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.Journal of medicinal chemistry, , Jul-09, Volume: 36, Issue:14, 1993
Discovery of a potent substance P antagonist: recognition of the key molecular determinant.Journal of medicinal chemistry, , Dec-25, Volume: 35, Issue:26, 1992
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
L-tryptophan urea amides as NK1/NK2 dual antagonists.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.Journal of medicinal chemistry, , Apr-29, Volume: 37, Issue:9, 1994
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.Journal of medicinal chemistry, , Jul-09, Volume: 36, Issue:14, 1993
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.Journal of medicinal chemistry, , Nov-26, Volume: 52, Issue:22, 2009
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Stereoselective synthesis of a novel 2-aza-7-oxabicyclo[3.3.0]octane as neurokinin-1 receptor antagonist.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 17, Issue:24, 2007
Successful virtual screening for a submicromolar antagonist of the neurokinin-1 receptor based on a ligand-supported homology model.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.Bioorganic & medicinal chemistry letters, , Feb-03, Volume: 8, Issue:3, 1998
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Novel, potent, and orally active substance P antagonists: synthesis and antagonist activity of N-benzylcarboxamide derivatives of pyrido[3,4-b]pyridine.Journal of medicinal chemistry, , Aug-04, Volume: 38, Issue:16, 1995
Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity.Journal of medicinal chemistry, , Dec-22, Volume: 38, Issue:26, 1995
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
Discovery of a potent substance P antagonist: recognition of the key molecular determinant.Journal of medicinal chemistry, , Dec-25, Volume: 35, Issue:26, 1992
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.Journal of medicinal chemistry, , Nov-26, Volume: 52, Issue:22, 2009
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
CNS drug design: balancing physicochemical properties for optimal brain exposure.Journal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK(1) receptor antagonist.Journal of medicinal chemistry, , Jul-05, Volume: 44, Issue:14, 2001
Quantitative structure-activity relationships (QSARs) of N-terminus fragments of NK1 tachykinin antagonists: a comparison of classical QSARs and three-dimensional QSARs from similarity matrices.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.Bioorganic & medicinal chemistry letters, , Feb-03, Volume: 8, Issue:3, 1998
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist cliniJournal of medicinal chemistry, , Feb-24, Volume: 54, Issue:4, 2011
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Discovery of novel, orally active dual NK1/NK2 antagonists.Bioorganic & medicinal chemistry letters, , Oct-22, Volume: 11, Issue:20, 2001
3-benzhydryl-4-piperidones as novel neurokinin-1 receptor antagonists and their efficient synthesis.Bioorganic & medicinal chemistry, , Sep-01, Volume: 19, Issue:17, 2011
Axially chiral 1,7-naphthyridine-6-carboxamide derivatives as orally active tachykinin NK(1) receptor antagonists: synthesis, antagonistic activity, and effects on bladder functions.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist.Journal of medicinal chemistry, , Jul-31, Volume: 46, Issue:16, 2003
Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propionBioorganic & medicinal chemistry letters, , Dec-03, Volume: 11, Issue:23, 2001
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14, 2013
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
The many roles for fluorine in medicinal chemistry.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 17, Issue:19, 2007
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
The many roles for fluorine in medicinal chemistry.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| tachykinin receptor activity | molecular function | Combining with a tachykinin neuropeptide and transmitting the signal across the membrane by activating an associated G-protein. [GOC:ai, GOC:bf, PMID:7639617, Wikipedia:Tachykinin] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| substance P receptor activity | molecular function | Combining with substance P, the peptide Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met, to initiate a change in cell activity. [GOC:mah, ISBN:0198506732] |
Located In
This protein is located in 7 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| sperm flagellum | cellular component | A microtubule-based flagellum (or cilium) that is part of a sperm, a mature male germ cell that develops from a spermatid. [GOC:cilia, GOC:sart, PMID:8441407] |
| cell body | cellular component | The portion of a cell bearing surface projections such as axons, dendrites, cilia, or flagella that includes the nucleus, but excludes all cell projections. [GOC:go_curators] |
| sperm head | cellular component | The part of the late spermatid or spermatozoon that contains the nucleus and acrosome. [PMID:22797892, PMID:24665388] |
| sperm midpiece | cellular component | The highly organized segment of the sperm flagellum which begins at the connecting piece and is characterized by the presence of 9 outer dense fibers (ODFs) that lie outside each of the 9 outer axonemal microtubule doublets and by a sheath of mitochondria that encloses the ODFs and the axoneme; the midpiece terminates about one-fourth of the way down the sperm flagellum at the annulus, which marks the beginning of the principal piece. [GOC:cjm, MP:0009831] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| sperm midpiece | cellular component | The highly organized segment of the sperm flagellum which begins at the connecting piece and is characterized by the presence of 9 outer dense fibers (ODFs) that lie outside each of the 9 outer axonemal microtubule doublets and by a sheath of mitochondria that encloses the ODFs and the axoneme; the midpiece terminates about one-fourth of the way down the sperm flagellum at the annulus, which marks the beginning of the principal piece. [GOC:cjm, MP:0009831] |
Involved In
This protein is involved in 38 target(s):
| Target | Category | Definition |
|---|
| aggressive behavior | biological process | A behavioral interaction between organisms in which one organism has the intention of inflicting physical damage on another individual. [GOC:hjd] |
| positive regulation of leukocyte migration | biological process | Any process that activates or increases the frequency, rate, or extent of leukocyte migration. [GOC:add] |
| angiotensin-mediated drinking behavior | biological process | The drinking behavior that is mediated by the action of angiotensin in the brain. Angiotensin stimulates the brain centers that control thirst. [GOC:mtg_cardio] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| tachykinin receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by tachykinin binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. Tachykinin is a short peptide with the terminal sequence (Phe-X-Gly-Leu-Met-NH2). [GOC:mah, PMID:14723970] |
| long-term memory | biological process | The memory process that deals with the storage, retrieval and modification of information a long time (typically weeks, months or years) after receiving that information. This type of memory is typically dependent on gene transcription regulated by second messenger activation. [http://hebb.mit.edu/courses/9.03/lecture4.html, ISBN:0582227089] |
| associative learning | biological process | Learning by associating a stimulus (the cause) with a particular outcome (the effect). [ISBN:0582227089] |
| detection of abiotic stimulus | biological process | The series of events in which an (non-living) abiotic stimulus is received by a cell and converted into a molecular signal. [GOC:hb] |
| response to ozone | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a ozone stimulus. [GOC:sm] |
| positive regulation of epithelial cell migration | biological process | Any process that activates or increases the frequency, rate or extent of epithelial cell migration. [GOC:BHF, GOC:dph, GOC:tb] |
| response to auditory stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an auditory stimulus. [GOC:BHF, GOC:dph, GOC:sl, GOC:tb] |
| regulation of smooth muscle cell migration | biological process | Any process that modulates the frequency, rate or extent of smooth muscle cell migration. [CL:0000192, GOC:mtg_muscle] |
| positive regulation of synaptic transmission, cholinergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of cholinergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter acetylcholine. [GOC:mah] |
| positive regulation of synaptic transmission, GABAergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of GABAergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter gamma-aminobutyric acid (GABA). [GOC:mah] |
| response to estradiol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123] |
| response to progesterone | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a progesterone stimulus. [GOC:sl] |
| response to nicotine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nicotine stimulus. [GOC:bf, GOC:ef, ISBN:0198506732, ISBN:0582227089] |
| operant conditioning | biological process | Learning to anticipate future events on the basis of past experience with the consequences of one's own behavior. [PMID:14662373] |
| sperm ejaculation | biological process | The expulsion of seminal fluid, thick white fluid containing spermatozoa, from the male genital tract. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
| eating behavior | biological process | The specific behavior of an organism relating to the intake of food, any substance (usually solid) that can be metabolized by an organism to give energy and build tissue. [GOC:jl, GOC:pr, PMID:19361967] |
| positive regulation of vascular permeability | biological process | Any process that increases the extent to which blood vessels can be pervaded by fluid. [GOC:jl] |
| response to ethanol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ethanol stimulus. [GOC:go_curators] |
| positive regulation of action potential | biological process | Any process that activates or increases the frequency, rate or extent of action potential creation, propagation or termination. This typically occurs via modulation of the activity or expression of voltage-gated ion channels. [GOC:go_curators] |
| positive regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is increased. [GOC:go_curators, GOC:mtg_cardio] |
| positive regulation of ossification | biological process | Any process that activates or increases the frequency, rate or extent of ossification, the formation of bone or of a bony substance or the conversion of fibrous tissue or of cartilage into bone or a bony substance. [GOC:go_curators] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| positive regulation of hormone secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of a hormone from a cell. [GOC:ai] |
| behavioral response to pain | biological process | Any process that results in a change in the behavior of an organism as a result of a pain stimulus. Pain stimuli cause activation of nociceptors, peripheral receptors for pain, include receptors which are sensitive to painful mechanical stimuli, extreme heat or cold, and chemical stimuli. [GOC:jid] |
| regulation of smooth muscle cell proliferation | biological process | Any process that modulates the frequency, rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc] |
| positive regulation of lymphocyte proliferation | biological process | Any process that activates or increases the rate or extent of lymphocyte proliferation. [GOC:ai] |
| positive regulation of epithelial cell proliferation | biological process | Any process that activates or increases the rate or extent of epithelial cell proliferation. [GOC:ai] |
| positive regulation of stress fiber assembly | biological process | Any process that activates or increases the frequency, rate or extent of the assembly of a stress fiber, a bundle of microfilaments and other proteins found in fibroblasts. [GOC:ai] |
| response to electrical stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an electrical stimulus. [GOC:ai] |
| smooth muscle contraction involved in micturition | biological process | The process leading to shortening and/or development of tension in the urinary bladder smooth muscle tissue involved in the expulsion urine from the body. [GOC:dph, PMID:15827347] |
| positive regulation of uterine smooth muscle contraction | biological process | Any process that increases the frequency, rate or extent of uterine smooth muscle contraction. [GOC:go_curators] |
| positive regulation of flagellated sperm motility | biological process | Any process that activates or increases the frequency, rate or extent of flagellated sperm motility. [GOC:cilia, GOC:jh2, GOC:krc, GOC:TermGenie, PMID:7513657] |