RVD-Hpα
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.[1] 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.[2] 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).[3][4]
species |
RVD-Hpα sequence |
human |
RVDPVNFKLLSH |
mouse |
RVDPVNFKLLSH |
rat |
RVDPVNFKfLSH |
consensus |
RVDPVNFKxLSH |
References
- ↑ 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. PMC 2154475 . PMID 18077343. doi:10.1073/pnas.0706980105.
- ↑ 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. PMC 2735371 . PMID 19380512. doi:10.1096/fj.09-132142.
- ↑ 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. PMC 3481297 . PMID 22952224. doi:10.1074/jbc.M112.382481.
- ↑ Macedonio G, Stefanucci A, Maccallini C, Mirzaie S, Novellino E, Mollica A. Hemopressin Peptides as Modulators of the Endocannabinoid System and their Potential Applications as Therapeutic Tools. Protein Pept Lett. 2016;23(12):1045-1051. PMID 27748182
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Phytocannabinoids | |
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Endocannabinoids | |
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Synthetic cannabinoids | Classical cannabinoids (dibenzopyrans) | |
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Non-classical cannabinoids | |
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Benzoylindoles | |
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Naphthoylindoles | |
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Naphthoylindazoles | |
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Pyrrolobenzoxazines | |
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Naphthylmethylindoles | |
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Phenylacetylindoles | |
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Indole-3-carboxamides | |
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Indole-3-carboxylates | |
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Tetramethylcyclo- propanoylindoles | |
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Indazole-3- carboxamides | |
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Tetramethylcyclo- propanoylindazoles | |
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Naphthoylpyrroles | |
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Eicosanoids | |
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Pyrazolecarboxamides | |
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Others | |
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Allosteric CBR ligands | |
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Endocannabinoid enhancers (inactivation inhibitors) | |
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Anticannabinoids (antagonists/inverse agonists/antibodies) | |
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Receptor (ligands) | CB1 |
- Antibodies: Brizantin (Бризантин)
- Dietressa (Диетресса)
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CB2 |
- Agonists: 2-AG
- 2-AGE (noladin ether)
- 3,3'-Diindolylmethane
- 4-O-Methylhonokiol
- α-Amyrin
- β-Amyrin
- A-796,260
- A-834,735
- A-836,339
- AM-1172
- AM-1221
- AM-1235
- AM-1241
- AM-2232
- Anandamide
- AZ-11713908
- Cannabinol
- Caryophyllene
- CB-13
- CBS-0550
- CP-55,940
- GW-405,833 (L-768,242)
- GW-842,166X
- HU-308
- JTE 7-31
- JWH-007
- JWH-015
- JWH-018
- JWH-73
- JWH-133
- L-759,633
- L-759,656
- Magnolol
- MDA-19
- Nabitan
- NADA
- PF-03550096
- S-444,823
- SER-601
- Serinolamide A
- UR-144
- Tedalinab
- THC (dronabinol)
- THCV
- Tetrahydromagnolol
- Virodhamine
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GPR18 | |
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GPR55 | |
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GPR119 | |
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Transporter (modulators) | |
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Enzyme (modulators) | FAAH | |
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MAGL | |
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ABHD6 |
- Inhibitors: JZP-169
- JZP-430
- KT182
- KT185
- KT195
- KT203
- LEI-106
- ML294
- ML295
- ML296
- UCM710
- WWL-70
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ABHD12 | |
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Others |
- Others: 2-PG (directly potentiates activity of 2-AG at CB1 receptor)
- ARN-272 (FAAH-like anandamide transporter inhibitor)
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- See also
- Receptor/signaling modulators
- Cannabinoids (cannabinoids by structure)
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