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Carfentanil binds very strongly to mu opioid receptors and acts as a competitive agonist.
Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex.
Carfentanil acts primarily on the mu (some kappa and delta) opioid receptors as an agonist. It will induce similar effects of analgesia as other opioids, however, due to its potency, it will also induce strong side effects such as sedation. Consequently, that is why it is used as a tranquilizer for large animals. Carfentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the brain, spinal cord, and other tissues. It exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Carfentanil also depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Carfentanil is an ultra-potent synthetic opioid. No human carfentanil metabolism data are available. Reportedly, Russian police forces used carfentanil and remifentanil to resolve a hostage situation in Moscow in 2002. This thus alleged use prompted interest in the pharmacology and toxicology of carfentanil in humans.We used Simulations Plus’s ADMET Predictor and Molecular Discovery’s MetaSite to predict possible metabolite formation.
Carfentanil binds very strongly to mu opioid receptors and acts as a competitive agonist. Hence, binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex.
narcotics, like oxycodone or hydrocodone, given to humans to treat pain. When even a fraction of the dose given to elephants is administered to humans, onset is rapid, difficult to stop, and hard to treat.
100 Grams, 200 Grams, 300 Grams, 500 grams, 1 Kg