Recent developments in 5-HT(1D) agonists
Related Experiment Video
Updated: Aug 15, 2026

Rapid In Situ Hybridization using Oligonucleotide Probes on Paraformaldehyde-prefixed Brain of Rats with Serotonin Syndrome
Published on: September 23, 2015
1Merck Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, CM20 2QR, UK. michael_russell@merck.com
Abstract:
Since the discovery of sumatriptan, several 5-HT(1D/1B) receptor agonists have now reached the clinic and marketplace as treatments for migraine. The highly efficacious F-11356 is the latest compound to emerge but none of these agents have appreciable selectivity between the h5-HT(1D) and h5-HT(1B) receptor subtypes. Research has now focused on obtaining selective h5-HT(1D) receptor agonists which, if inhibition of peptide release is involved in the antimigraine action, may be expected to have reduced vasoconstrictor liability. This has led especially to the discovery of L-775606 and PNU-109291, which should constitute useful tools to delineate the role of h5-HT(1D) receptors in migraine.
Related Concept Videos
Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists
Adrenergic Agonists: Indirect-Acting Agents
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...
Direct-Acting Cholinergic Agonists: Pharmacological Actions
Drugs Affecting GI Tract Motility: Dopamine Receptor Antagonists
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Direct-Acting Cholinergic Agonists: Therapeutic Uses
