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

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

1973 • 12,522 citations

Ethical guidelines for investigations of experimental pain in conscious animals

1983 • 7,639 citations

SOME QUANTITATIVE USES OF DRUG ANTAGONISTS

1959 • 3,948 citations

The formalin test: A quantitative study of the analgesic effects of morphine, meperidine, and brain stem stimulation in rats and cats

1977 • 2,494 citations

Synthetic analgesics. II. Dithienylbutenyl- and dithienylbutylamines.

1953 • 1,702 citations

Local effector functions of capsaicin-sensitive sensory nerve endings: Involvement of tachykinins, calcitonin gene-related peptide and other neuropeptides

1988 • 1,673 citations

Neurotransmitter functions of mammalian tachykinins.

1993 • 1,101 citations

[3H]Ketanserin (R 41 468), a selective 3H-ligand for serotonin2 receptor binding sites. Binding properties, brain distribution, and functional role.

1982 • 1,049 citations

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

1991 • 875 citations

Receptors and antagonists for substance P and related peptides.

1994 • 622 citations

Specific in vitro and in vivo binding of 3H-raclopride a potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain

1985 • 503 citations

A Method for Evaluating both Non-Narcotic and Narcotic Analgesics

1957 • 493 citations

[³H]8‐Hydroxy‐2‐(Di‐n‐Propylamino)Tetralin Binding to Pre‐ and Postsynaptic 5‐Hydroxytryptamine Sites in Various Regions of the Rat Brain

1985 • 458 citations

Neuropeptides in the Respiratory Tract: Part I

1991 • 453 citations

A substance P antagonist inhibits vagally induced increase in vascular permeability and bronchial smooth muscle contraction in the guinea pig

1983 • 443 citations

Multiple opioid receptors: ligand selectivity profiles and binding site signatures.

1989 • 441 citations

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

1991 • 429 citations

Vascular protein leakage in various tissues induced by substance P, capsaicin, bradykinin, serotonin, histamine and by antigen challenge

1983 • 429 citations

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

1993 • 376 citations

New selective agonists for neurokinin receptors: pharmacological tools for receptor characterization

1988 • 360 citations

Cutaneous stimuli releasing immunoreactive substance P in the dorsal horn of the cat

1988 • 348 citations

THE PEPTIDES: Analysis, Synthesis, Biology

1981 • 274 citations

Structure, expression, and some regulatory mechanisms of the rat preprotachykinin gene encoding substance P, neurokinin A, neuropeptide K, and neuropeptide gamma

1990 • 227 citations

Characterization of neuropeptide‐induced histamine release from human dispersed skin mast cells

1988 • 216 citations

Pharmacology of CP-99,994; a nonpeptide antagonist of the tachykinin neurokinin-1 receptor.

1993 • 215 citations

Substance P and Neurokinins

1987 • 200 citations

Substance P and Neurokinins

1987 • 197 citations

Pharmacological profile of a high affinity dipeptide NK₁ receptor antagonist, FK888

1992 • 146 citations

[3H]-BRL 43694 (granisetron), a specific ligand for 5-HT3 binding sites in rat brain cortical membranes

1989 • 138 citations

Effects and interactions of sensory neuropeptides on airway microvascular leakage in guinea‐pigs

1988 • 134 citations

Relative potencies of neurokinins in guinea pig trachea and human bronchus

1987 • 124 citations

Guanine nucleotide regulation of agonist interactions at [3H]SCH23390-labeled D1 dopamine receptors in rat striatum

1986 • 115 citations

Binding characteristics and affinity labeling of protein constituents of the human IM-9 lymphoblast receptor for substance P.

1986 • 100 citations

HISTAMINE H₁‐RECEPTORS IN THE BRAIN OF THE GUINEA‐PIG AND THE RAT: DIFFERENCES IN LIGAND BINDING PROPERTIES AND REGIONAL DISTRIBUTION

1980 • 100 citations

Enantioselective inhibition of ampomorphine-induced emesis in the ferret by the neurokinin1 receptor antagonist CP-99,994

1994 • 94 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

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

The rising sun shines on substance P and related peptides

1993 • 66 citations

Neurokinin receptor subtypes characterized by biological assays

1994 • 65 citations

Capsaicin Increases Airflow Resistance in Guinea PigsIn Vivoby Activating both NK₂and NK₁Tachykinin Receptors

1993 • 64 citations

Comparison of Several Methods for Isolation of Rat Peritoneal Mast Cells.

1966 • 41 citations

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

1994 • 34 citations

The Use of Ligand Binding for the Characterisation of α-Adrenoceptors

1980 • 31 citations

FR 113680: a novel tripeptide substance P antagonist with NK¹ receptor selectivity

1992 • 30 citations

Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs

1993 • 12 citations

Degradation of Rat Brain Cholinergic Muscarinic Receptors In Vitro: Enhancement by Agonists and Inhibition by Antagonists

1985 • 8 citations

Estimation of blood levels of endothelin and neurokinin receptor antagonists at the rat portal and jugular veins after oral administration as a tool in peptide drug design.

1994 • 6 citations

Differential Protection and Selective Deprotection in Peptide Synthesis

1981 • 4 citations