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]
species |
RVD-Hpα sequence |
human |
RVDPVNFKLLSH |
mouse |
RVDPVNFKLLSH |
rat |
RVDPVNFKfLSH |
consensus |
RVDPVNFKxLSH |
References
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Phytocannabinoids |
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Cannabinoid
metabolites |
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Endogenous
cannabinoids |
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Synthetic
cannabinoid
receptor
agonists |
Classical
cannabinoids
(Dibenzopyrans) |
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Nonclassical
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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Tetramethylcyclopropanoylindoles |
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Indazole-3-carboxamides |
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Tetramethylcyclopropanoylindazoles |
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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
modulators of
cannabinoid
receptors |
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Endocannabinoid
activity enhancers |
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Cannabinoid
receptor
antagonists and
inverse agonists |
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Receptor
(ligands) |
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- 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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Transporter
(modulators) |
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Enzyme
(modulators) |
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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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