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Pharmacological properties of GR38032F, a novel antagonist at 5‐HT3 receptors
TLDR
R,S‐GR38032F is highly selective for 5‐HT3 receptors, and at concentrations of 3 × 10‐6‐3 × 10−5m, had negligible agonist or antagonist activity on other 5‐ HT or non‐5‐HT receptor‐containing tissues on which it was tested. Expand
Anti-emetic profile of a non-peptide neurokinin NK1 receptor antagonist, CP-99,994, in ferrets.
TLDR
The anti-emetic effects of a NK1 receptor antagonist (racemic CP-99,994) in the ferret was effective against a range of emetogens, comprising cytotoxic drugs, radiation, morphine, ipecacuanha and copper sulphate. Expand
Structure‐activity relationships for some substance P‐related peptides that cause wheal and flare reactions in human skin.
TLDR
The results are discussed in relation to the mechanism of the ‘axon reflex’ vasodilatation in skin that is thought to involve mast cells in addition to substance P‐containing primary afferent neurones. Expand
Receptor-selective, peptidase-resistant agonists at neurokinin NK-1 and NK-2 receptors: New tools for investigating neurokinin function
TLDR
In the anaesthetised rat, the NK-1 agonist, GR73632 was more potent than SP, NKA or NKB at causing the histamine-independent extravasation of plasma proteins into the skin after intradermal administration. Expand
Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor.
TLDR
Replacement of D-Trp9 by D-Pro9 in the nonselective neurokinin antagonist SP(5-11) gave a partial agonist withNK-2 receptor selectivity, which produced a potent inhibition of NK-2 agonist-induced bronchoconstriction in the anaesthetized guinea-pig. Expand
Neurotransmitters, drugs and disease
TLDR
Applied neuropharmacology: Introduction Parkinsonism dementias schizophrenia epilepsy anxiety, anxiolytic-hypnotics depression painanalgesics, and more. Expand
Effect of 5‐HT3 receptor antagonists on responses to selective activation of mesolimbic dopaminergic pathways in the rat
TLDR
These results are in agreement with the proposed facilitatory role of 5‐HT3 receptor activation on mesolimbic dopaminergic transmission, and suggest that 5‐ HT3 antagonists may have important therapeutic indications for the treatment of CNS disorders in which mesolimmeric dopamine systems are perturbed. Expand
The effects of substance P on histamine and 5‐hydroxytryptamine release in the rat
TLDR
1. Substance P (SP) induces histamine release from isolated rat peritoneal mast cells at concentrations of 0·1‐10 μM and this results in a down-regulation in the secretion of histamine in response to EMT. Expand
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