Neuromedin U receptors

Overview

Neuromedin U receptors are activated by the endogenous 25 amino acid peptide neuromedin U (neuromedin U-25, NmU-25), a peptide originally isolated from pig spinal cord [1]. In humans, NmU-25 appears to be the sole product of a precursor gene (NMU, P48645) showing a broad tissue distribution, but which is expressed at highest levels in the upper gastrointestinal tract, CNS, bone marrow and fetal liver. Much shorter versions of NmU are found in some species, but not in human, and are derived at least in some instances from the proteolytic cleavage of the longer NmU. Despite species differences in NmU structure, the C-terminal region (particularly the C-terminal pentapeptide) is highly conserved and contains biological activity. Neuromedin S (neuromedin S-33) has also been identified as an endogenous agonist [2]. NmS-33 is, as its name suggests, a 33 amino-acid product of a precursor protein derived from a single gene and contains an amidated C-terminal heptapeptide identical to NmU. NmS-33 appears to activate NMU receptors with equivalent potency to NmU-25.

References

  1. Minamino N, Kangawa K, Matsuo H. Neuromedin U-8 and U-25: novel uterus stimulating and hypertensive peptides identified in porcine spinal cord. Biochem Biophys Res Commun 1985;130:1078-85.
  2. Mori K, Miyazato M, Ida T, et al. Identification of neuromedin S and its possible role in the mammalian circadian oscillator system. EMBO J 2005;24:325-35.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Human
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Human non-orphan GPCRs
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Reference agonist:
NMU‐23
EC50:
1.3 nM
Human
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Assay modes:
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Panels:
Human non-orphan GPCRs
à la carte
Reference agonist:
NMU‐23
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390 pM
Mouse
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Agonist
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Mouse non-orphan GPCRs
à la carte
Reference agonist:
NMU‐23
EC50:
2.2 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
NMU‐23
EC50:
350 pM