SMP0000675
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Diphenoxylate Action Pathway
Diphenoxylate (also known as Difenossilato or Lomotil) is analgesic that can bind to mu-type opioid receptor to activate associated G-protein in the sensory neurons of central nervous system (CNS), which will reduce the level of intracellular cAMP by inhibiting adenylate cyclase. The binding of diphenoxylate will eventually lead to reduced pain because of decreased nerve conduction and release of neurotransmitter. Hyperpolarization of neuron is caused by inactivation of calcium channels and activation of potassium channels via facilitated by G-protein.
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Drug Action
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SMP0000676
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Dezocine Action Pathway
Dezocine (also known as Dalgan) is analgesic that can bind to mu-type opioid receptor to activate associated G-protein in the sensory neurons of central nervous system (CNS), which will reduce the level of intracellular cAMP by inhibiting adenylate cyclase. The binding of dezocine will eventually lead to reduced pain because of decreased nerve conduction and release of neurotransmitter. Hyperpolarization of neuron is caused by inactivation of calcium channels and activation of potassium channels via facilitated by G-protein.
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Drug Action
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SMP0000677
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Levomethadyl Acetate Action Action Pathway
Levomethadyl acetate (also known as LAAM) is a synthetic synthetic opioid analgesic with multiple actions quantitatively similar to those as morphine, the most prominent of which involve the central nervous system and organs composed of smooth muscle. However, levomethadyl acetate is more active and more toxic than morphine. Levomethadyl acetate can bind to mu-type opioid receptor to activate associated G-protein in the sensory neurons of central nervous system (CNS), which will reduce the level of intracellular cAMP by inhibiting adenylate cyclase. The binding of levomethadyl acetate will eventually lead to reduced pain because of decreased nerve conduction and release of neurotransmitter. Therefore, methadyl acetate can reduce nerve conduction and decrease neurotransmitter release; so that perception of pain signals can be blocked. Levomethadyl acetate can also open calcium-dependent inwardly rectifying potassium channels (OP1 receptor agonist) to reduce neuronal excitability as well as lead to hyperpolarization.
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Drug Action
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SMP0000678
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Methadyl Acetate Action Pathway
Methadyl Acetate (also known as Acetylmethadol) is a synthetic opioid analgesic that can bind to mu-type opioid receptor to activate associated G-protein in the sensory neurons of central nervous system (CNS), which will reduce the level of intracellular cAMP by inhibiting adenylate cyclase. The binding of methadyl acetate will eventually lead to reduced pain because of decreased nerve conduction and release of neurotransmitter. Therefore, methadyl acetate can reduce nerve conduction and decrease neurotransmitter release; so that perception of pain signals can be blocked.
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Drug Action
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SMP0000679
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3-Methylthiofentanyl Action Pathway
Methadyl Acetate (also known as Acetylmethadol) is analgesic that can bind to mu-type opioid receptor to activate associated G-protein in the sensory neurons of central nervous system (CNS), which will reduce the level of intracellular cAMP by inhibiting adenylate cyclase. The binding of methadyl acetate will eventually lead to reduced pain because of decreased nerve conduction and release of neurotransmitter. Hyperpolarization of neuron is caused by inactivation of calcium channels and activation of potassium channels via facilitated by G-protein.
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Drug Action
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SMP0000680
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Dimethylthiambutene Action Pathway
Dimethylthiambutene (also known as Ohton or Aminobutene) is an opioid analgesic and substrate for mu-type opioid receptor which can be used for relieving pain. Dimethylthiambutene can act on mu-opiod receptor on neurons located at central nervous system. Binding of dimethylthiambutene on mu-type opioid receptor can activate associated G(i) proteins, which inhibits adenylate cyclase and reduce intracellular cAMP level. G(i) protein can also open potassium channels and close calcium channels to result in hyperpolarize on neuron. Binding of dimethylthiambutene on mu-type opioid receptor will eventually relieving the pain by reducing nerve conduction and neurotransmitter release.
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Drug Action
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SMP0000681
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Ethylmorphine Action Pathway
Ethylmorphine (also known as codethyline and dionine) is an opioid analgesic. Ethylmorphine can be metabolized to form morphine by cytochrome P450 2D6 (CYP2D6). Morphine can bind the mu-type opioid receptor on central nervous system (CNS) to reduce the pain. Morphine can also bind and inhibit gamma-Aminobutyric acid (GABA) inhibitory interneurons. These interneurons can inhibit the descending pain inhibition pathway; therefore, without the interneurons, pain modulation will go downstream.
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Drug Action
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SMP0000682
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Leucine Stimulation on Insulin Signaling
The branched chain amino acid (BCAA) leucine is able to signal transduction pathways that modulate translation initiation for protein synthesis in skeleton muscles. In the presence of leucine, hyperphosphorylation of 4E-BP1 causes its affinity for eIF4E to be lowered. This allows eIF4F protein complexes to recognize, unfold and guide the mRNA to the 43S preinitiation complex thereby increasing translation initiation. In addition, leucine has a transient affect on the release of insulin and/or enhances sensitivity of muscle cells to insulin. A culmination of both signals at the mammalian target of rapamycin (mTOR) and perhaps other signaling, such as PKCĪ“, are needed for maximum translation initiation to occur.
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Signaling
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SMP0000683
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Levallorphan Action Pathway
Levallorphan (also known as Lorfan and Naloxifan) is a type of medication that can be used for treating drug overdoses and respirotry depression. Levallorphan can bind to mu-type opioid receptor and kappa-type opioid receptor on neuron of central nerves system (CNS). Effects of opioids such as respiratory depression, hypotension and sedation can be prevented or reversed by levallorphan. Levallorphan can also be used for treating pentazocine which is a type of psychotomimetic and dysphoric effects of agonist-antagonists.
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Drug Action
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SMP0000684
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Buprenorphine Action Pathway
Buprenorphine, trade name subutex, suboxone, zubsolv and bunavail, is a partial agonist of mu-opioid receptors and a kappa-opioid receptor antagonist and is prescribed for opioid addiction to prevent cravings and symptoms of withdrawal. The binding of these receptors causes hyperpolarization and decreased neuronal excitability. Buprenorphine has a longer duration of action due to its slow dissociation from the receptor. This long rate of action causes a long clinical effect and decreases physical dependence. Buprenorphine can also prevent opioid use by inhibiting exogenous opioid effects. This elimination of the rush from the opioid can block the reinforcing behaviour of the drug and may treat opioid addiction. Buprenorphine is available on its own or in combination with naloxone.
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Drug Action
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