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Neuropeptides: opportunities for drug discovery
Tomas Hökfelt1, Tamas Bartfai, Floyd Bloom
1Department of Neuroscience, Karolinska Institute, Stockholm, Sweden. tomas.hokfelt@neuro.ki.se
The Lancet. Neurology
|July 25, 2003
Summary
Neuropeptides are crucial signaling molecules in the nervous system, acting as neurotransmitters, hormones, and messengers. Their diverse roles and numerous receptors offer significant potential for developing new drugs targeting nervous system disorders.
Area of Science:
- Neuroscience
- Pharmacology
- Molecular Biology
Background:
- Neuropeptides and their G-protein-coupled receptors are widely distributed and complement classic neurotransmitters.
- Their functions span neurotransmission, hormonal regulation, and immune signaling, with particular importance during nervous system challenges like stress or injury.
Purpose of the Study:
- To highlight the therapeutic potential of neuropeptides and their receptors for nervous system disorders.
- To review the current landscape of neuropeptide receptor ligand development.
Main Methods:
- Literature review of neuropeptide research over 30 years.
- Analysis of neuropeptide and receptor distribution and function.
- Examination of clinical trial data for neuropeptide receptor ligands.
Main Results:
- Neuropeptides play diverse roles, including neurotransmitter, hormone, and immune messenger functions.
- Evidence suggests neuropeptides are critical during nervous system stress, injury, or drug abuse.
- A substance P receptor antagonist (neurokinin 1) shows clinical efficacy for depression and emesis.
Conclusions:
- The abundance of neuropeptides and their receptors presents numerous drug discovery opportunities for neurological and psychiatric conditions.
- Several neuropeptide receptor ligands are in clinical trials, indicating promising therapeutic avenues.