adrenergic drug

• アドレナリン受容体刺激薬、アドレナリン作用薬

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adrenergic、adrenergic agent、adrenergic agonist、adrenergic receptor agonist、adrenergics

WordNet

1. use recreational drugs (同)do drugs
2. administer a drug to; "They drugged the kidnapped tourist" (同)dose
3. a substance that is used as a medicine or narcotic
4. drug that has the effects of epinephrine (同)adrenergic_drug
5. relating to epinephrine (its release or action) (同)sympathomimetic

PrepTutorEJDIC

1. 『薬』,薬品,薬剤 / 『麻薬』,麻酔剤 / 〈人〉‘に'薬(特に麻酔剤)を与える / 〈飲食物〉‘に'(麻酔薬・毒薬などの)薬を混ぜる

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/05/05 22:22:35」(JST)

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Epinephrine

Norepinephrine

Dopamine

Chemical structures of catecholamines.

Sympathomimetic drugs mimic the effects of transmitter substances of the sympathetic nervous system such as catecholamines, epinephrine (adrenaline), norepinephrine (noradrenaline), dopamine, etc. Such drugs are used to treat cardiac arrest and low blood pressure, or even delay premature labor, among other things.

These drugs act at the postganglionic sympathetic terminal, either directly activating postsynaptic receptors, blocking breakdown and reuptake, or stimulating production and release of catecholamines.

Mechanisms of action

The mechanisms of sympathomimetic drugs can be direct-acting, such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting, such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors.

Direct-acting

Adrenergic receptor agonists

Main article: Adrenergic agonist

Direct stimulation of the α- and β-adrenergic receptors can produce sympathomimetic effects. Salbutamol is a very commonly used direct-acting β₂-agonist. Other examples include phenylephrine, isoproterenol, and dobutamine.

Dopaminergic agonists

Stimulation of the D1 receptor by dopaminergic agonists such as fenoldopam is used intravenously to treat hypertensive crisis.

Indirect-acting

Norepinephrine transporter blockade

Classical sympathomimetic drugs are amphetamines (including MDMA), ephedrine, and cocaine, which act by blocking and reversing norepinephrine transporter (NET) activity. NET is a transport protein expressed on the surface of some cells that clears noradrenaline and adrenaline from the extracellular space and into cells, terminating the signaling effects.

Structure Activity Relationship

A primary or secondary aliphatic amine separated by 2 carbons from a substituted benzene ring is minimally required for high agonist activity. The pKa of the amine is approximately 8.5-10. 1- Substitution on aromatic ring-

The presence of hydroxy group in the benzene ring at 3rd and 4th position shows maximum alpha and beta activity

Cross-reactivity

Substances like cocaine also affect dopamine, and some substances like MDMA affect serotonin.

Norepinephrine is synthesized by the body into epinephrine, causing central nervous system stimulation. Thus, all sympathomimetic amines fall into the larger group of stimulants (see psychoactive drug chart). Many of these stimulants have therepeutic use and abuse potential, can induce tolerance, and possibly physical dependence.

Comparison

"Parasympatholytic" and "sympathomimetic" are similar, but not identical. For example, both cause mydriasis, but parasympatholytics reduce accommodation (cycloplegia) while sympathomimetics do not.

Examples

• ephedrine (found in Ephedra)
• pseudoephedrine (also found in Ephedra species)
• amphetamine
• methamphetamine
• methylphenidate (Ritalin)
• lisdexamfetamine (Vyvanse)
• cocaine (found in Erythroxylum coca, Coca)
• cathinone (found in Catha edulis, Khat)
• cathine (also found in Catha edulis)
• methcathinone
• benzylpiperazine (BZP)
• methylenedioxypyrovalerone (MDPV)
• 4-methylaminorex
• pemoline (Cylert)
• phenmetrazine (Preludin)
• propylhexedrine (Benzedrex)

See also

• Sympathetic nervous system

References

External links

• MeSH Amines,+Sympathomimetic
• Sympathomimetic+amine at eMedicine Dictionary
• Sympathomimetic at eMedicine Dictionary

UpToDate Contents

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• 5. アルコールおよびその他の薬物の有害な使用のスクリーニング screening for unhealthy use of alcohol and other drugs

English Journal

• Intercepting neoplastic progression in lung malignancies via the beta adrenergic (β-AR) pathway: Implications for anti-cancer drug targets.

• Al-Wadei HA, Ullah MF, Al-Wadei MH.SourceExperimental Oncology Laboratory, Department of Biomedical and Diagnostic Sciences, University of Tennessee, Knoxville, TN 37996, USA; Sana'a University, Sana'a, Republic of Yemen.
• Pharmacological research : the official journal of the Italian Pharmacological Society.Pharmacol Res.2012 Jul;66(1):33-40. Epub 2012 Apr 2.
• The understanding of signaling cascades involved in the induction, promotion, and progression of cancer, although advanced in recent years, is still incomplete. Tracing the imbalance of the impaired, physiologically-essential cellular signaling that drives the neoplastic process is a complex issue.
• PMID 22487140

• Mechanical responsiveness of the endothelial cell of Schlemm's canal: scope, variability and its potential role in controlling aqueous humour outflow.

• Zhou EH, Krishnan R, Stamer WD, Perkumas KM, Rajendran K, Nabhan JF, Lu Q, Fredberg JJ, Johnson M.SourceProgram in Molecular and Integrative Physiological Sciences, Department of Environmental Health, Harvard School of Public Health, , Boston, MA, USA.
• Journal of the Royal Society, Interface / the Royal Society.J R Soc Interface.2012 Jun 7;9(71):1144-55. Epub 2011 Dec 14.
• Primary open-angle glaucoma is associated with elevated intraocular pressure, which in turn is believed to result from impaired outflow of aqueous humour. Aqueous humour outflow passes mainly through the trabecular meshwork (TM) and then through pores formed in the endothelium of Schlemm's canal (SC
• PMID 22171066

Japanese Journal

• COPE Trial

• 梅本 誠治,松？ 益？,荻原 俊男 [他]
• 循環器内科 70(4), 413-420, 2011-10
• NAID 40019059926

• Fluorescence ratiometric detection of ligand-induced receptor internalization using extracellular coiled-coil tag-probe labeling.

• Yano Yoshiaki,Matsuzaki Katsumi
• FEBS letters 585(14), 2385-2388, 2011-07-21
• … The N-terminus of the β2-adrenergic receptor expressed on the cell surface was doubly labeled with pH-sensitive fluorescein and pH-insensitive tetramethylrhodamine. … This simple and accurate method of detecting the agonistic activity of receptors will be useful for high-throughput screening of drug candidates. …
• NAID 80021902638

Related Links

• Adrenergic Drugs - Elmhurst College

Adrenergic nerves release norepinephrine as the neurotransmitter for the sympathetic nervous system. The sympathetic system activates and prepares the body for vigorous muscular activity, stress, and emergencies. Adrenergic drugs ...

• Adrenergic Drugs II - Elmhurst College

Adrenergic drugs stimulate the adrenergic nerves directly by mimicking the action of norepinephrine. Therapeutically, these drugs are used in nasal decongestants as the main example given here. The structures of the stimulants closely mimic ...

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リンク元	「アドレナリン受容体刺激薬」「adrenergic agonist」「adrenergic receptor agonist」「adrenergic agent」
関連記事	「adrenergics」「adrenergic」「drug」

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adrenergic receptor agonist、adrenergic agonist、adrenergic drug、adrenergics

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アドレナリン作動薬、アドレナリン作用薬、アドレナリン模倣薬、アドレナリン受容体作動薬、アドレナリン刺激薬

「adrenergic agonist」

　　[★]

• アドレナリン受容体刺激薬、アドレナリン作動薬、アドレナリン刺激薬、アドレナリン作用薬

関

adrenergic、adrenergic agent、adrenergic drug、adrenergic receptor agonist、adrenergics、adrenomimetic

「adrenergic receptor agonist」

　　[★]

• アドレナリン受容体刺激薬、アドレナリン受容体作動薬

関

adrenergic agonist、adrenergic drug、adrenergics、adrenomimetic

「adrenergic agent」

　　[★]

• アドレナリン系薬物、アドレナリン作用薬

関

adrenergic、adrenergic agonist、adrenergic drug、adrenergics

「adrenergics」

　　[★]

アドレナリン受容体刺激薬、アドレナリン作用薬

関

adrenergic、adrenergic agent、adrenergic agonist、adrenergic drug、adrenergic receptor agonist

「adrenergic」

　　[★]

• adj.

• アドレナリンの、アドレナリン性の

　 　

「drug」

　　[★]

同

drugs