RVD-Hpα is an endogenous neuropeptide found in human and mammalian brain, which was originally proposed to act as a selective agonist for the CB1 cannabinoid receptor. It is a 12-amino acid polypeptide having the amino acid sequence Arg-Val-Asp-Pro-Val-Asn-Phe-Lys-Leu-Leu-Ser-His and is an N-terminal extended form of hemopressin, a 9-AA polypeptide derived from the α1 subunit of hemoglobin which has previously been shown to act as a CB1 inverse agonist. All three polypeptides have been isolated from various mammalian species, with RVD-Hpα being one of the more abundant neuropeptides expressed in mouse brain, and these neuropeptides represent a new avenue for cannabinoid research distinct from the previously known endogenous lipid-derived cannabinoid agonists such as anandamide. Recently it was shown that RVD-Hpα (also called Pepcan-12) is a potent negative allosteric modulator at CB1 receptors, together with other newly described N-terminally extended peptides (pepcans).
|| RVD-Hpα sequence|
- ↑ Heimann, A.; Gomes, I.; Dale, C.; Pagano, R.; Gupta, A.; De Souza, L.; Luchessi, A.; Castro, L.; Giorgi, R.; Rioli, V.; Ferro, E. S.; Devi, L. A. (2007). "Hemopressin is an inverse agonist of CB1 cannabinoid receptors". Proceedings of the National Academy of Sciences of the United States of America. 104 (51): 20588–20593. Bibcode:2007PNAS..10420588H. doi:10.1073/pnas.0706980105. PMC 2154475. PMID 18077343.
- ↑ Gomes, I.; Grushko, J.; Golebiewska, U.; Hoogendoorn, S.; Gupta, A.; Heimann, A.; Ferro, E.; Scarlata, S.; Fricker, L.; Devi, L. A. (2009). "Novel endogenous peptide agonists of cannabinoid receptors". The FASEB Journal. 23 (9): 3020–3029. doi:10.1096/fj.09-132142. PMC 2735371. PMID 19380512.
- ↑ Bauer, M.; Chicca, A.; Tamborrini, M.; Eisen, D.; Lerner, R.; Lutz, B.; Poetz, O.; Pluschke, G.; Gertsch, J. (2012). "Identification and Quantification of a New Family of Peptide Endocannabinoids (Pepcans) Showing Negative Allosteric Modulation at CB1 Receptors". Journal of Biological Chemistry. 287 (44): 36944–36967. doi:10.1074/jbc.M112.382481. PMC 3481297. PMID 22952224.