DB01571 - 3-Methylfentanyl
| Identification | |
|---|---|
| Name | 3-Methylfentanyl |
| Accession Number | DB01571 |
| Type | small molecule |
| Description | 3-Methylfentanyl (3-MF, mefentanyl) is an opioid analgesic that is an analogue of fentanyl. 3-Methylfentanyl is one of the most potent drugs that has been widely sold on the black market, estimated to be between 400-6000 times stronger than morphine depending on which isomer is used (with cis isomer being the more potent one). 3-Methylfentanyl was first discovered in 1974 [4] and subsequently appeared on the street as an alternative to the clandestinely produced fentanyl analogue ?-methylfentanyl. However it quickly became apparent that 3-methylfentanyl was much more potent than ?-methylfentanyl, and corespondingly even more dangerous. [Wikipedia] |
| Structure |
|
| Categories (*) | |
| Molecular Weight | 350.4971 |
| Groups | illicit |
| Monoisotopic Weight | 350.235813592 |
| Pharmacology | |
| Indication | Not Available |
| Mechanism of action | Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Fentanyl's analgesic activity is, most likely, due to its conversion to morphine. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability. |
| Absorption | Not Available |
| Protein binding | Not Available |
| Biotransformation | Not Available |
| Route of elimination | Not Available |
| Toxicity | 3-Methylfentanyl has resulted in many deaths among opiate addicts using the drug. |
| Affected organisms |
|
| Interactions | |
| Drug Interactions | Not Available |
| Food Interactions | Not Available |
Targets
| Mu-type opioid receptor | |
|---|---|
| Name | Mu-type opioid receptor |
| Gene Name | OPRM1 |
| Pharmacological action | yes |
| Actions | agonist |
| References |
|
| DTHybrid score | 0.9578 |
| Delta-type opioid receptor | |
| Name | Delta-type opioid receptor |
| Gene Name | OPRD1 |
| Pharmacological action | yes |
| Actions | agonist |
| References |
|
| DTHybrid score | 0.7831 |
| Kappa-type opioid receptor | |
| Name | Kappa-type opioid receptor |
| Gene Name | OPRK1 |
| Pharmacological action | yes |
| Actions | agonist |
| References |
|
| DTHybrid score | 0.7602 |