まとめ
モルフィンはネズミの脳でドーパミンを増加させ,その濃度は下垂体とストライアトゥームで高くなります. モルヒンに対する耐性は,炭素14をドーパミンとノレアピネフリンに組み込むことを2倍にします.
科学分野:
- 神経科学は神経科学である.
- 薬理学 薬理学とは
背景:
- モルフィンはオピオイド鎮痛剤で,神経伝達物質システムに知られている効果があります.
- ドーパミンとノレアピネフリンの代謝にモルヒンの影響を理解することは,その作用機構と耐性発達を理解するために重要である.
研究 の 目的:
- ネズミの脳領域におけるドーパミンとノレピネフリンの蓄積にモルヒネ投与の影響を調査する.
- モルヒン耐性と耐性のないネズミの神経伝達物質代謝を比較する.
主な方法:
- ネズミにモルヒンを内静脈経由で投与した.
- 放射性炭素14でラベル付けされたチロシンは,ドーパミンとノレピネフリンの合成を追跡するために使用されました.
- 視床下部とストライアタムを含む脳領域は,特定の時間点での放射性マーケルの神経伝達物質の蓄積について分析されました.
主要な成果:
- 耐性のないラットでは,モルヒンの投与により,ドーパミンの蓄積が増加し,1時間後にヒポタラマスとストライアトゥームでピークに達しました.
- 耐性のあるネズミは,モルヒンの単一投与を受けたネズミと比較して,これらの脳領域で[[[14]C]ドーパミンと[14]C]ノレアピネフリンの組み込み率の2倍以上を示した.
結論:
- モルフィンはネズミの脳におけるドーパミンとノレピネフリンの代謝を著しく変化させる.
- モルヒン耐性は,重要な脳の領域におけるドーパミンとノレアピネフリンの転移率の顕著な増加と関連しています.
関連する概念動画
Adrenergic Neurons: Neurotransmission
Postganglionic sympathetic fibers (except those supplying the sweat glands) releasing noradrenaline or norepinephrine are called noradrenergic or adrenergic neurons. Noradrenaline, dopamine, adrenaline, or epinephrine are collectively called "catecholamines" as they contain a catechol moiety and an amine side chain. The five stages of neurotransmitter release involve their synthesis, storage, release, reuptake and metabolism.
Synthesis: Catecholamine synthesis requires tyrosine, which is taken...
Synthesis: Catecholamine synthesis requires tyrosine, which is taken...
Adrenergic Agonists: Indirect-Acting Agents
Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Drugs Affecting Neurotransmitter Release or Uptake
Certain drugs can affect how neurotransmitters called catecholamines, are released or taken back up in the adrenergic neuron. They can have different effects on the body's sympathetic transmission. Reserpine, a natural compound found in the Rauwolfia shrub, blocks a transporter called vesicular monoamine transporter (VMAT), which leads to a buildup of catecholamines in the cell and reduces sympathetic transmission. Another drug called guanethidine works in multiple ways, including blocking...
Drugs Affecting Neurotransmitter Synthesis
Drugs affecting neurotransmitter synthesis can impact the adrenergic neuron and the synthesis of neurotransmitters. For example, α-methyltyrosine and carbidopa target specific enzymes involved in catecholamine synthesis. α-methyltyrosine inhibits the enzyme tyrosine hydroxylase, which converts tyrosine into dopamine. By blocking this enzyme, α-methyltyrosine reduces dopamine production and other catecholamines. Carbidopa, on the other hand, inhibits the enzyme dopa decarboxylase, which converts...
CNS Stimulants: Cocaine, Amphetamines and Cannabinoids
CNS stimulants, such as cocaine, amphetamines, and cannabinoids, have varying structures and mechanisms of action that lead to different therapeutic effects and side effects. Cocaine, with its molecular formula C17H21NO4, is a tropane alkaloid and a tertiary amino compound. It has two chemical forms: the hydrochloride salt and the "freebase." The former is in powder form, while the latter involves removing the hydrochloride salt to create a form that can be smoked. Cocaine exerts its effects by...


