| Content Provider |
World Health Organization (WHO)-Global Index Medicus |
| Author |
Méndez-Díaz, Mónica Amancio-Belmont, Octavio Hernández-Vázquez, Eduardo Ruiz-Contreras, Alejandra E. Hernández-Luis, Francisco Prospéro-García, Oscar |
| Description |
Author Affiliation: Méndez-Díaz M ( Grupo de Neurociencias de la UNAM, Laboratorio de Canabinoides, Departamento de Fisiología, Facultad de Medicina, Universidad Nacional Autónoma de México, México, D. F. 04510 Mexico.); Amancio-Belmont O ( Grupo de Neurociencias de la UNAM, Laboratorio de Canabinoides, Departamento de Fisiología, Facultad de Medicina, Universidad Nacional Autónoma de México, México, D. F. 04510 Mexico.); Hernández-Vázquez E ( Grupo de Neurociencias de la UNAM, Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, México, D. F. 04510 Mexico.); Ruiz-Contreras AE ( Grupo de Neurociencias de la UNAM, Laboratorio de Neurogenómica Cognitiva, Coordinación de Psicofisiología, Facultad de Psicología, Universidad Nacional Autónoma de México, México, D. F. 04510 Mexico.); Hernández-Luis F ( Grupo de Neurociencias de la UNAM, Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, México, D. F. 04510 Mexico.); Prospéro-García O ( Grupo de Neurociencias de la UNAM, Laboratorio de Canabinoides, Departamento de Fisiología, Facultad de Medicina, Universidad Nacional Autónoma de México, México, D. F. 04510 Mexico. Electronic address: opg@unam.mx.) |
| Abstract |
Over the past decade, pharmacological manipulation of cannabinoid 1 receptor (CB1R) has become an interesting approach for the management of food ingestion disorders, among other physiological functions. Searching for new substances with similar desirable effects, but fewer side-effects we have synthesized a SR141716A (a cannabinoid receptor inverse agonist also called Rimonabant) analog, 1-(2,4-Difluorophenyl)-4-methyl-N-(1-piperidinyl)-5-[4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide, ENP11, that so far, as we have previously shown, has induced changes in glucose availability, i.e. hypoglycemia, in rats. In this study we tested the effects, if any, of ENP11 (0.5, 1.0, and 3.0mg/kg) in food ingestion, core temperature, pain perception and motor control in adult Wistar rats. Results showed that ENP11 reduced food ingestion during the first hour immediately after administration. Likewise, ENP11 (1.0mg/kg) blocked anandamide (AEA)-induced hyperphagia during the first 4h of the dark phase of the light-dark cycle, and it also blocked AEA-induced hypothermia. However, none of the ENP11 doses used affected pain perception or motor control. We believe that ENP11 is a potential useful CB1R antagonist that reduces food ingestion and regulates core temperature. |
| File Format |
HTM / HTML |
| ISSN |
00913057 |
| Volume Number |
135 |
| e-ISSN |
18735177 |
| Journal |
Pharmacology Biochemistry and Behavior |
| Language |
English |
| Publisher |
Elsevier |
| Publisher Date |
2015-08-01 |
| Publisher Place |
United States |
| Access Restriction |
One Nation One Subscription (ONOS) |
| Subject Keyword |
Discipline Behavioral Sciences Discipline Biochemistry Discipline Pharmacology Appetite Depressants Pharmacology Cannabinoid Receptor Antagonists Feeding Behavior Drug Effects Piperidines Pyrazoles Receptor, Cannabinoid, Cb1 Antagonists & Inhibitors Animals Arachidonic Acids Body Temperature Body Weight Eating Endocannabinoids Hyperphagia Chemically Induced Drug Therapy Psychology Male Pain Pain Perception Polyunsaturated Alkamides Postural Balance Rats Rats, Wistar Journal Article Research Support, Non-u.s. Gov't |
| Content Type |
Text |
| Resource Type |
Article |
| Subject |
Biological Psychiatry Behavioral Neuroscience Biochemistry Clinical Biochemistry Toxicology Pharmacology |
