The tachykinin NK1 receptor. Part I: Ligands and mechanisms of cellular activation

A Potent Nonpeptide Antagonist of the Substance P (NK ₁ ) Receptor

1991 • 875 citations

Peptides: Chemistry, structure and biology

1977 • 799 citations

Tachykinin receptors and tachykinin receptor antagonists

1993 • 649 citations

Receptors and antagonists for substance P and related peptides.

1994 • 622 citations

The mammalian tachykinin receptors

1995 • 496 citations

Molecular characterization of a functional cDNA for rat substance P receptor

1989 • 463 citations

A potent and selective non-peptide antagonist of the neurokinin a (NK2) receptor

1992 • 441 citations

Pharmacological properties of a potent and selective nonpeptide substance P antagonist.

1991 • 429 citations

In vitro and in vivo biological activities of SR140333, a novel potent non-peptide tachykinin NK1 receptor antagonist

1993 • 376 citations

Molecular Characterization of a Functional cDNA Encoding the Rat Substance P Receptor

1990 • 355 citations

Tachykinin receptor types: Classification and membrane signalling mechanisms

1991 • 342 citations

Pharmacological receptors for substance P and neurokinins

1987 • 337 citations

Rapid endocytosis of a G protein-coupled receptor: substance P evoked internalization of its receptor in the rat striatum in vivo.

1995 • 292 citations

Multiple tachykinin binding sites in peripheral tissues and in brain

1986 • 276 citations

Direct linkage of three tachykinin receptors to stimulation of both phosphatidylinositol hydrolysis and cyclic AMP cascades in transfected Chinese hamster ovary cells.

1992 • 259 citations

Differential activation of intracellular effector by two isoforms of human neurokinin-1 receptor.

1992 • 242 citations

Selective agonists for substance P and neurokinin receptors

1987 • 239 citations

Nonpeptidal peptidomimetics with .beta.-D-glucose scaffolding. A partial somatostatin agonist bearing a close structural relationship to a potent, selective substance P antagonist

1992 • 221 citations

Activity and Distribution of Binding Sites in Brain of a Nonpeptide Substance P (NK ₁ ) Receptor Antagonist

1991 • 221 citations

Discovery of a potent substance P antagonist: recognition of the key molecular determinant

1992 • 220 citations

Different binding epitopes on the NK1 receptor for substance P and a non-peptide antagonist

1993 • 213 citations

Delineation of the endocytic pathway of substance P and its seven-transmembrane domain NK1 receptor.

1995 • 209 citations

Backbone cyclization: A new method for conferring conformational constraint on peptides

1991 • 202 citations

Substance P and Neurokinins

1987 • 200 citations

Substance P and Neurokinins

1987 • 197 citations

Localization of agonist and antagonist binding domains of the human neurokinin-1 receptor.

1992 • 190 citations

Biological evaluation of substance P antagonists

1984 • 189 citations

Amino–aromatic interaction between histidine 197 of the neurokinin-1 receptor and CP 96345

1993 • 185 citations

Molecular cloning, structural characterization and functional expression of the human substance P receptor

1991 • 178 citations

Human substance P receptor (NK-1): organization of the gene, chromosome localization and functional expression of cDNA clones

1991 • 178 citations

The substance P receptor, which couples to Gq/11, is a substrate of beta-adrenergic receptor kinase 1 and 2

1993 • 178 citations

Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP-96,345 and RP67580.

1992 • 175 citations

Conversion of antagonist-binding site to metal-ion site in the tachykinin NK-1 receptor

1995 • 167 citations

Species differences in affinities of non-peptide antagonists for substance p receptors

1991 • 163 citations

Potent and highly selective neurokinin antagonists

1990 • 160 citations

The substance P receptor antagonist CP-96,345 interacts with Ca2+ channels

1992 • 160 citations

Mechanisms of desensitization and resensitization of G protein-coupled neurokinin1 and neurokinin2 receptors.

1996 • 154 citations

Agonist-induced internalization of the substance P (NK1) receptor expressed in epithelial cells

1994 • 144 citations

Interaction of Substance P with the Second and Seventh Transmembrane Domains of the Neurokinin-1 Receptor

1994 • 136 citations

Pertussis toxin-insensitive G protein mediates substance P-induced inhibition of potassium channels in brain neurons.

1988 • 126 citations

Piperidine-ether based hNK1 antagonists 1: Determination of the relative and absolute stereochemical requirements

1994 • 124 citations

Determination of the amino acid residues in substance P conferring selectivity and specificity for the rat neurokinin receptors.

1992 • 121 citations

Molecular basis for the species selectivity of the substance P antagonist CP-96,345.

1993 • 118 citations

The tachykinin NK1 receptor antagonist CP-99,994 attenuates cisplatin induced emesis in the ferret

1993 • 109 citations

Peripheral effects of neurokinins: functional evidence for the existence of multiple receptors

1987 • 108 citations

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 antagonist

1992 • 108 citations

Tachykinin peptides affect differently the second messenger pathways after binding to CHO-expressed human NK-1 receptors.

1996 • 105 citations

Mutations along transmembrane segment II of the NK-1 receptor affect substance P competition with non-peptide antagonists but not substance P binding.

1994 • 105 citations

The Tachykinin Receptors

1994 • 99 citations

Biochemical Characterization of Two Different Forms of the Substance P Receptor in Rat Submaxillary Gland

1993 • 91 citations

Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor.

1994 • 90 citations

The substance P receptor antagonist CP-96,345 interacts with Ca2+ channels

1992 • 88 citations

Ligand Binding Kinetics of Substance P and Neurokinin A Receptors Stably Expressed in Chinese Hamster Ovary Cells and Evidence for Differential Stimulation of Inositol 1,4,5‐Trisphosphate and Cyclic AMP Second Messenger Responses

1992 • 86 citations

[pGlu6, Pro9]SP6-11, a selective agonist for the substance P P-receptor subtype

1986 • 85 citations

Synthesis and Biological Properties of Enzyme‐Resistant Analogues of Substance P

1981 • 83 citations

Homologous desensitization of substance-P-induced inositol polyphosphate formation in rat parotid acinar cells

1987 • 83 citations

Multiple intracellular signaling pathways of the neuropeptide substance P receptor

1992 • 79 citations

Molecular Mechanism of Action of Non-peptide Ligands for Peptide Receptors

1995 • 78 citations

Novel, Potent, and Orally Active Substance P Antagonists: Synthesis and Antagonist Activity of N-Benzylcarboxamide Derivatives of Pyrido[3,4-b]pyridine

1995 • 74 citations

N-Acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists

1993 • 73 citations

Spantide II, an effective tachykinin antagonist having high potency and negligible neurotoxicity.

1990 • 72 citations

Characterization of CP-122,721; a nonpeptide antagonist of the neurokinin NK1 receptor.

1996 • 71 citations

Two nonpeptide tachykinin antagonists act through epitopes on corresponding segments of the NK1 and NK2 receptors.

1993 • 69 citations

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

1996 • 67 citations

N-Heteroaryl-2-phenyl-3-(benzyloxy)piperidines: A Novel Class of Potent Orally Active Human NK₁ Antagonists

1996 • 66 citations

Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles

1992 • 65 citations

Neuropharmacological characterization of SR 140333, a non peptide antagonist of NK1 receptors

1994 • 62 citations

The role of histidine 265 in antagonist binding to the neurokinin-1 receptor.

1994 • 61 citations

Synthesis of Potent Cyclic Hexapeptide NK-1 Antagonists. Use of a Minilibrary in Transforming a Peptidal Somatostatin Receptor Ligand into an NK-1 Receptor Ligand via a Polyvalent Peptidomimetic

1996 • 60 citations

Synthesis and Biological Activity of NK-1 Selective, N-Backbone Cyclic Analogs of the C-Terminal Hexapeptide of Substance P

1996 • 59 citations

Tryptophan-Derived NK1 Antagonists: Conformationally Constrained Heterocyclic Bioisosteres of the Ester Linkage

1995 • 59 citations

Differential expression of two isoforms of the neurokinin-1 (substance P) receptor in vivo

1996 • 58 citations

Identification of L-Tryptophan Derivatives with Potent and Selective Antagonist Activity at the NK1 Receptor

1994 • 57 citations

Human Epidermal Growth Factor (EGF) Receptor Sequence Recognized by EGF Competitive Monoclonal Antibodies

1989 • 55 citations

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

1995 • 54 citations

Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK₁ antagonists

1993 • 51 citations

3-Aryl-1,2-diacetamidopropane Derivatives as Novel and Potent NK-1 Receptor Antagonists

1996 • 49 citations

Interaction of glutamine 165 in the fourth transmembrane segment of the human neurokinin-1 receptor with quinuclidine antagonists.

1994 • 49 citations

The species selectivity of chemically distinct tachykinin nonpeptide antagonists is dependent on common divergent residues of the rat and human neurokinin-1 receptors.

1994 • 48 citations

Chemical Cross-Linking of the Substance P (NK-1) Receptor to the α Subunits of the G Proteins G_q and G₁₁

1996 • 47 citations

Two Signal Transduction Mechanisms of Substance P‐induced Depolarization in Locus Coeruleus Neurons

1993 • 45 citations

Characterization of the substance P receptor-mediated calcium influx in cDNA transfected Chinese hamster ovary cells. A possible role of inositol 1,4,5-trisphosphate in calcium influx

1994 • 43 citations

Multiple mechanisms of arachidonic acid release in Chinese hamster ovary cells transfected with cDNA of substance P receptor

1994 • 43 citations

Identification of a Series of 3-(Benzyloxy)-1-azabicyclo[2.2.2]octane Human NK1 Antagonists

1995 • 42 citations

Molecular cloning of the murine substance K and substance P receptor genes

1992 • 42 citations

Rational design of high affinity tachykinin NK1 receptor antagonists

1994 • 42 citations

Specific residues at the top of transmembrane segment V and VI of the neurokinin-1 receptor involved in binding of the nonpeptide antagonist CP 96,345 [corrected]

1994 • 42 citations

Tachykinin Antagonists

1995 • 42 citations

Chloride channels in myocytes from rabbit colon are regulated by a pertussis toxin-sensitive G protein

1993 • 41 citations

Tetrazole NK1 receptor antagonists: The identification of an exceptionally potent orally active antiemetic compound

1996 • 40 citations

Isolation and characterisation of the human lung NK-1 receptor cDNA

1991 • 40 citations

Attenuation of agonist‐induced desensitization of the rat substance P receptor by progressive truncation of the C‐terminus

1994 • 36 citations

Regulation of Substance P Receptor Affinity by Guanine Nucleotide‐Binding Proteins

1989 • 35 citations

Conformational Compatibility as a Basis of Differential Affinities of Tachykinins for the Neurokinin-1 Receptor

1995 • 35 citations

Synthesis of RPR 100893, prototype of a new series of potent and selective non peptide NK1 antagonists : the triarylperhydroisoindolols.

1994 • 34 citations

Conserved His^VI‐17 of the NK‐1 receptor is involved in binding of non‐peptide antagonists but not substance P

1993 • 34 citations

Functional nonequivalence of structurally homologous domains of neurokinin-1 and neurokinin-2 type tachykinin receptors

1993 • 34 citations

Conformationally constrained tachykinin analogs: potent and highly selective neurokinin NK-2 receptor agonists

1992 • 33 citations

In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist.

1996 • 33 citations

Capsaicin‐induced inhibition of motility of the rat isolated vas deferens: do multiple neuropeptides mediate the visceromotor effects of capsaicin?

1987 • 33 citations

WS9326A, a novel tachykinin antagonist isolated from Streptomyces violaceusniger No. 9326. II Biological and pharmacological properties of WS9326A and tetrahydro-WS9326A (FK224).

1992 • 33 citations

Molecular cloning of substance P receptor cDNA from guinea-pig uterus

1992 • 32 citations

Piperidine-ether based hNK1 antagonists 2: Investigation of the effect of N-substitution

1995 • 32 citations

SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist

1996 • 31 citations

Quinuclidine-based NK-1 antagonists I: 3-benzyloxy-1-azabicyclo[2.2.2]octanes

1993 • 30 citations

Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors

1996 • 30 citations

Acyclic NK-1 antagonists: 2-benzhydryl-2-aminoethyl ethers

1994 • 29 citations

Importance of Parallel Vectors and "Hydrophobic Collapse" of the Aligned Aromatic Rings: Discovery of a Potent Substance P Antagonist

1994 • 28 citations

Gem-disubstituted amino-ether based substance p antagonists

1994 • 28 citations

Rational design of high affinity tachykinin NK2 receptor antagonists

1994 • 28 citations

Both extracellular and transmembrane residues contribute to the species selectivity of the neurokinin-1 receptor antagonist WIN 51708.

1994 • 28 citations

Molecular determinants of the species selectivity of neurokinin type 1 receptor antagonists.

1995 • 28 citations

Studies on neurokinin antagonists. 2. Design and structure-activity relationships of novel tripeptide substance P antagonists, N.alpha.-[N.alpha.-(N.alpha.-acetyl-L-threonyl)-N1-formyl-D-tryptophyl]-N-methyl-N-(phenylmethyl)-L-phenylalaninamide and its related compounds

1992 • 27 citations

Synthesis and Biological Evaluation of NK1 Antagonists Derived from L-Tryptophan

1995 • 27 citations

Thapsigargin blocks the mobilisation of intracellular calcium caused by activation of human NK1 (long) receptors expressed in chinese hamster ovary cells

1993 • 25 citations

The design of a dipeptide library for screening at peptide receptor sites

1993 • 25 citations

Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists

1992 • 24 citations

Cyclic peptides as selective tachykinin antagonists

1993 • 24 citations

4,4-Disubstituted Piperidines: A New Class of NK1 Antagonists

1995 • 22 citations

Aza-Tricyclic Substance P Antagonists

1994 • 21 citations

Substance P stimulation of polyphosphoinositide hydrolysis in rat anterior pituitary membranes involves a GTP-dependent mechanism

1991 • 21 citations

A water-soluble, stable dipeptide NK1 receptor-selective neurokinin receptor antagonist with potent in vivo pharmacological effects: S18523

1996 • 20 citations

Protein kinase C mediates delayed inhibitory feedback regulation of human neurokinin type 1 receptor activation of phospholipase C in UC11 astrocytoma cells.

1994 • 20 citations

Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists

1991 • 19 citations

Quinuclidine based NK-1 antagonists 2: determination of the absolute stereochemical requirements

1993 • 19 citations

Modulation of membrane K+ conductance in T-lymphocytes by substance P via a GTP-binding protein

1989 • 19 citations

Characterization of the interaction of diacylpiperazine antagonists with the human neurokinin-1 receptor: identification of a common binding site for structurally dissimilar antagonists.

1995 • 18 citations

Synthesis and substance P antagonist activity of naphthimidazolium derivatives

1992 • 17 citations

An SAR study for the non-peptide substance P receptor (NK1) antagonist, CP-96,345.

1992 • 16 citations

Articulating a pharmacophore driven synthetic strategy: Discovery of a potent substance P antagonist

1994 • 15 citations

Studies on Neurokinin Antagonists. 4. Synthesis and Structure-Activity Relationships of Novel Dipeptide Substance P Antagonists: N2-[(4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl]-N-methyl-N-(phenylmethyl)-3-(2-naphthyl)-L-alaninamide and Its Related Compounds

1994 • 15 citations

Regulation of the responses to gonadotropin-releasing hormone, muscarine and substance P in sympathetic neurons by changes in cellular constituents and intracellular application of peptide fragments of the substance P receptor.

1994 • 15 citations

Highly potent substance P antagonists substituted with β-phenyl- or β-benzyl-proline at position 10

1994 • 14 citations

Synthesis and biological evaluation of novel NK‐1 tachykinin receptor antagonists: The use of cycloalkyl amino acids as a template

1995 • 14 citations

Studies on neurokinin antagonists. 3. Design and structure-activity relationships of new branched tripeptides N.alpha.-(substituted L-aspartyl, L-ornithyl, or L-lysyl)-N-methyl-N-(phenylmethyl)-L-phenylalaninamides as substance P antagonists

1993 • 14 citations

Phenyl-glycinol based NK1 receptor antagonists — towards the minimum pharmacophore

1995 • 14 citations

1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists.

1993 • 13 citations

1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists

1995 • 12 citations

Spiro-piperidine non-peptide neurokinin-1 receptor antagonists

1995 • 10 citations

N-alkyl quinuclidinium substance P antagonists

1994 • 10 citations

Residue 78 in the second transmembrane domain of the neurokinin-1 receptor is important in coupling high affinity agonist binding to multiple second messenger responses.

1995 • 10 citations

Synthesis of a benzo[b]-1,5-naphthyridine derivative as a potential constrained NK1 receptor antagonist

1994 • 10 citations

Synthesis of a potent antagonist of substance P by replacing the CH₂SCH₃ and the α‐carboxamide groups of the methionine al [Orn⁶]‐SP_6–11 by benzyl ester groups

1993 • 10 citations

Nuclear variations of quinuclidine substance P antagonists: 2-diphenylmethyl-1-azabicyclo[3.2.2]nonan-3-amines

1993 • 10 citations

Synthesis of conformationally restricted substance P antagonists

1995 • 10 citations

2-Aryl-1-azabicyclo[2.2.2]octanes as novel nonpeptide substance P antagonists

1994 • 9 citations

Synthesis and in vitro activities of new tryptophan-modified and thiomethylene-containing pseudopeptide antagonists of the neurokinins

2009 • 9 citations

Structure-Activity Relationships of Agonist and Antagonist Ligands

1994 • 9 citations

Morphan based substance P antagonists

1996 • 7 citations

1,2,4-Triacylpiperidine substance p antagonists: Separation of affinities for the NK-1 receptor and the L-type calcium channel

1995 • 6 citations

Indolizidine derivatives as potential substance P antagonists

1996 • 6 citations

Linear amides as substance P antagonists

1996 • 6 citations

4,4-Diphenyl-7-perhydrothiapyrano[3,4-c]pyrrolone, a new series of substance P receptors antagonists

1995 • 4 citations

Synthesis of substance-P C-terminal hexapeptide analogues and their biological activity. Analogues with antagonistic activity without containing d-amino acids

1994 • 2 citations

ChemInform Abstract: Studies on Neurokinin Antagonists. Part 4. Synthesis and Structure‐ Activity Relationships of Novel Dipeptide Substance P Antagonists: N2‐( (4R)‐4‐Hydroxy‐1‐((1‐methyl‐1H‐indol‐3‐yl)carbonyl)‐L‐prolyl)‐N‐methyl‐ N‐(phenylmethyl)‐3‐(2‐naphthyl)‐L‐alaninamide and Its Related Compounds.

1994 • 2 citations