RIMONABANT IS THE FIRST IN A NEW CLASS OF AGENTS THAT ACT BY SELECTIVELY BLOCKING THE CANNABINOID-1 RECEPTORS WITH RESULTANT CENTRAL AND METABOLIC PERIPHERAL EFFECTS, THEREBY DECREASING FOOD INTAKE AND INCREASES ENERGY EXPENDITURE. CB1 RECEPTORS ARE PRESENT BOTH IN THE CNS AS WELL AS IN CERTAIN PERIPHERAL TISSUES LIKE ADIPOCYTES, GASTROINTESTINAL TRACT AND LIVER. RIMONABANT IS REPORTED TO POSSESS A 1000-FOLD HIGHER AFFINITY FOR THE CB1 RECEPTOR THAN CB2 RECEPTOR. IT SHOWS HIGH AFFINITY FOR THE CENTRALLY LOCATED CANNABINOID RECEPTOR, WHILE DISPLAYING LOW AFFINITY FOR THE PERIPHERALLY LOCATED RECEPTOR. ADDITIONALLY, IT HAS LITTLE OR NO AFFINITY FOR NON-CANNABINOID RECEPTORS.
* ACTION OF RIMONABANT ON CNS ( BRAIN ) CB1 RECEPTORS
" DECREASED FOOD INTAKE
" DECREASED TOBACCO DEPENDENCE
* ACTION OF RIMONABANT ON PERIPHERAL TISSUE (ADIPOCYTES) CB1 RECEPTORS
" DECREASED INSULIN RESISTANCE
" DECREASED TRIGLYCERIDES
" INCREASED GLUCOSE TOLERANCE
" INCREASED HDL-CHOLESTEROL
" INCREASED ADIPONECTIN