RGD Reference Report - Hemopressin is an inverse agonist of CB1 cannabinoid receptors. - Rat Genome Database

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Hemopressin is an inverse agonist of CB1 cannabinoid receptors.

Authors: Heimann, Andrea S  Gomes, Ivone  Dale, Camila S  Pagano, Rosana L  Gupta, Achla  de Souza, Laura L  Luchessi, Augusto D  Castro, Leandro M  Giorgi, Renata  Rioli, Vanessa  Ferro, Emer S  Devi, Lakshmi A 
Citation: Heimann AS, etal., Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20588-93. doi: 10.1073/pnas.0706980105. Epub 2007 Dec 12.
RGD ID: 152025530
Pubmed: PMID:18077343   (View Abstract at PubMed)
PMCID: PMC2154475   (View Article at PubMed Central)
DOI: DOI:10.1073/pnas.0706980105   (Journal Full-text)

To date, the endogenous ligands described for cannabinoid receptors have been derived from membrane lipids. To identify a peptide ligand for CB(1) cannabinoid receptors, we used the recently described conformation-state sensitive antibodies and screened a panel of endogenous peptides from rodent brain or adipose tissue. This led to the identification of hemopressin (PVNFKFLSH) as a peptide ligand that selectively binds CB(1) cannabinoid receptors. We find that hemopressin is a CB(1) receptor-selective antagonist, because it is able to efficiently block signaling by CB(1) receptors but not by other members of family A G protein-coupled receptors (including the closely related CB(2) receptors). Hemopressin also behaves as an inverse agonist of CB(1) receptors, because it is able to block the constitutive activity of these receptors to the same extent as its well characterized antagonist, rimonabant. Finally, we examine the activity of hemopressin in vivo using different models of pain and find that it exhibits antinociceptive effects when administered by either intrathecal, intraplantar, or oral routes, underscoring hemopressin's therapeutic potential. These results represent a demonstration of a peptide ligand for CB(1) cannabinoid receptors that also exhibits analgesic properties. These findings are likely to have a profound impact on the development of novel therapeutics targeting CB(1) receptors.

Gene Ontology Annotations    Click to see Annotation Detail View

Molecular Function
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
G protein-coupled receptor binding enablesIDA 152025530; 152025530PMID:18077343UniProt 
peptidase activity enablesIDA 152025530PMID:18077343UniProt 

Objects Annotated

Genes (Rattus norvegicus)
Ace  (angiotensin I converting enzyme)
Hba-a1  (hemoglobin alpha, adult chain 1)
Hba-a2  (hemoglobin alpha, adult chain 2)


Additional Information