0000000000559950

AUTHOR

Simon M. Luckman

showing 2 related works from this author

Central functional response to the novel peptide cannabinoid, hemopressin.

2013

Hemopressin is the first peptide ligand to be described for the CB₁ cannabinoid receptor. Hemopressin acts as an inverse agonist in vivo and can cross the blood-brain barrier to both inhibit appetite and induce antinociception. Despite being highly effective, synthetic CB₁ inverse agonists are limited therapeutically due to unwanted, over dampening of central reward pathways. However, hemopressin appears to have its effect on appetite by affecting satiety rather than reward, suggesting an alternative mode of action which might avoid adverse side effects. Here, to resolve the neuronal circuitry mediating hemopressin's actions, we have combined blood-oxygen-level-dependent, pharmacological-ch…

AM251MaleCannabinoid receptorHypothalamus MiddleNerve Tissue ProteinsNucleus accumbensSatiety ResponseRats Sprague-DawleyCellular and Molecular Neurosciencechemistry.chemical_compoundHemoglobinsMiceRandom AllocationPiperidinesReceptor Cannabinoid CB1Appetite DepressantsmedicineInverse agonistAnimalsPeriaqueductal GrayPharmacologyMice KnockoutNeuronsBehavior AnimalCannabinoidsHemopressinPeptide FragmentsRatsVentral tegmental areamedicine.anatomical_structurechemistryPyrazolesRaphe NucleiBrain stimulation rewardRaphe nucleiPsychologyNeuroscienceInjections Intraperitonealmedicine.drugNeuropharmacology
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The Peptide Hemopressin Acts through CB1Cannabinoid Receptors to Reduce Food Intake in Rats and Mice

2010

Hemopressin is a short, nine amino acid peptide (H-Pro-Val-Asn-Phe-Lys-Leu-Leu-Ser-His-OH) isolated from rat brain that behaves as an inverse agonist at the cannabinoid receptor CB1, and is shown here to inhibit agonist-induced receptor internalization in a heterologous cell model. Since this peptide occurs naturally in the rodent brain, we determined its effect on appetite, an established central target of cannabinoid signaling. Hemopressin dose-dependently decreases night-time food intake in normal male rats and mice, as well as in obeseob/obmale mice, when administered centrally or systemically, without causing any obvious adverse side effects. The normal, behavioral satiety sequence is …

LeptinMaleTime FactorsCannabinoid receptormedicine.medical_treatmentPharmacologyRats Sprague-DawleyEatingHemoglobinsMicechemistry.chemical_compoundPiperidinesReceptor Cannabinoid CB1RimonabantChlorocebus aethiopsDronabinolReceptorMice KnockoutBehavior AnimalDrug Administration RoutesGeneral NeuroscienceArticlesEndocannabinoid systemCircadian RhythmProtein TransportCOS CellsRimonabantmedicine.drugAgonistmedicine.medical_specialtymedicine.drug_classMorpholinesGreen Fluorescent ProteinsDrinking BehaviorHyperphagiaNaphthalenesBiologyTransfectionInternal medicinemedicineAnimalsInverse agonistAnalysis of VariancePsychotropic DrugsDose-Response Relationship DrugCyclohexanolsPeptide FragmentsHemopressinBenzoxazinesRatsMice Inbred C57BLEndocrinologychemistryPyrazolesCannabinoidFood DeprivationThe Journal of Neuroscience
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