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Distribution, physiology and pharmacology of relaxin-3/RXFP3 systems in brain

Ma, S, Smith, Craig, Blasiak, A and Gundlach, AL 2016, Distribution, physiology and pharmacology of relaxin-3/RXFP3 systems in brain, British journal of pharmacology, vol. 174, pp. 1-15, doi: 10.1111/bph.13659.

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Title Distribution, physiology and pharmacology of relaxin-3/RXFP3 systems in brain
Author(s) Ma, S
Smith, CraigORCID iD for Smith, Craig
Blasiak, A
Gundlach, AL
Journal name British journal of pharmacology
Volume number 174
Start page 1
End page 15
Total pages 15
Publisher Wiley-Blackwell
Place of publication Chichester, Eng.
Publication date 2016-10-23
ISSN 1476-5381
Keyword(s) Science & Technology
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Summary Relaxin-3 is a member of a superfamily of structurally-related peptides that includes relaxin and insulin-like peptide hormones. Soon after the discovery of the relaxin-3 gene, relaxin-3 was identified as an abundant neuropeptide in brain with a distinctive topographical distribution within a small number of GABAergic neuron populations that is well conserved across species. Relaxin-3 is thought to exert its biological actions through a single class-A GPCR - relaxin-family peptide receptor 3 (RXFP3). Class-A comprises GPCRs for relaxin-3 and insulin-like peptide-5 and other peptides such as orexin and the monoamine transmitters. The RXFP3 receptor is selectively activated by relaxin-3, whereas insulin-like peptide-5 is the cognate ligand for the related RXFP4 receptor. Anatomical and pharmacological evidence obtained over the last decade supports a function of relaxin-3/RXFP3 systems in modulating responses to stress, anxiety-related and motivated behaviours, circadian rhythms, and learning and memory. Electrophysiological studies have identified the ability of RXFP3 agonists to directly hyperpolarise thalamic neurons in vitro, but there are no reports of direct cell signalling effects in vivo. This article provides an overview of earlier studies and highlights more recent research that implicates relaxin-3/RXFP3 neural network signalling in the integration of arousal, motivation, emotion and related cognition, and that has begun to identify the associated neural substrates and mechanisms. Future research directions to better elucidate the connectivity and function of different relaxin-3 neuron populations and their RXFP3-positive target neurons in major experimental species and humans are also identified.
Language eng
DOI 10.1111/bph.13659
Field of Research 110999 Neurosciences not elsewhere classified
1115 Pharmacology And Pharmaceutical Sciences
Socio Economic Objective 920199 Clinical Health (Organs
HERDC Research category C1 Refereed article in a scholarly journal
ERA Research output type C Journal article
Copyright notice ©2016, British Pharmacological Society
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Document type: Journal Article
Collection: School of Medicine
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