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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.

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Description

BUY CARFENTANIL ONLINE

Carfentanyl is an analog of the synthetic opioid analgesic fentanyl. A unit of carfentanil is 100 times as potent as the same amount of fentanyl. Carfentanil was first synthesized in 1974 by a team of chemists at Janssen Pharmaceutica which included Paul Janssen. It has a quantitative potency approximately 10,000 times that of morphine and 100 times that of fentanyl, with activity in humans starting at about 1 microgram. Currently sufentanil, approximately 10–20 times less potent (500 to 1000 times the efficacy of morphine per weight) than carfentanil, is the maximum strength fentanyl analog for use in humans.

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Buy carfentanil powder online Carfentanil or carfentanyl is an analog of the synthetic opioid analgesic fentanyl. It is 10,000 times more potent than morphine, making it among the most potent commercially used opioids. The toxicity of carfentanil in humans and its ready commercial availability has aroused concerns over its potential use as a weapon of mass destruction by rogue nations and terrorist groups Carfentanil is the most potent commercial opioid in the world, according to the US Drug Enforcement Agency (DEA). Its chemically similar cousin fentanyl is up to 50 times stronger the heroin and carfentanil is 100 times stronger than fentanyl itself. Before being discovered by drug dealers,

Pharmacology

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.

Metabolism/Metabolites

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.

Mechanism of Action

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.

How Does Carfentanil Affect Humans?

Because of carfentanil’s potency, the effects on the human body and brain are very rapid. Even in elephants, the sedative effects are especially rapid. According to Elephant Care International, veterinarians must watch elephants for signs of pulmonary edema and capillary bleeding, characterized by a pink foam issuing from the elephant’s trunk, which indicates a potentially fatal rise in blood pressure. While doses administered to elephants are specifically to knock the animal
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.
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