alpha-adrenergic agonist

• αアドレナリン受容体刺激薬、αアドレナリン作動薬、αアドレナリン刺激薬

WordNet

1. first in order of importance; "the alpha male in the group of chimpanzees"; "the alpha star in a constellation is the brightest or main star"
2. the 1st letter of the Greek alphabet
3. the beginning of a series or sequence; "the Alpha and Omega, the first and the last, the beginning and the end"--Revelations
4. early testing stage of a software or hardware product; "alpha version"
5. (biochemistry) a drug that can combine with a receptor on a cell to produce a physiological reaction
6. a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist"
7. someone involved in a contest or battle (as in an agon)
8. drug that has the effects of epinephrine (同)adrenergic_drug
9. relating to epinephrine (its release or action) (同)sympathomimetic

PrepTutorEJDIC

1. アルファ(ギリシア語アルファベットの第1字A,α;英語のA,aに相当) / アルファ星(星座の主星)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/05/18 08:05:07」(JST)

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[Wiki en表示]

Alpha Adrenergic agonist
Drug class
Skeletal structor formula of phenylephrine, a common nasel decongestant
Use	Decongestant, Hypotension, Bradycardia, Hypothermia etc.
Biological target	Alpha adrenergic receptors of the α subtype
ATC code	N07
External links
MeSH	D012141

An adrenergic alpha-agonist (or alpha-adrenergic agonists) are a class sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The alpha-adrenergic receptor has two subclasses α₁ and α₂. Alpha 2 receptors are associated with sympatholytic properties. α Adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity. The activation of α₁ and α₂ inhibits the enzyme Adenylate cyclase. This in turn leads to the inactivation of the secondary messenger Cyclic adenosine monophosphate and induces smooth muscle and blood vessel constriction.

Classes

noradrenaline

Although complete selectivity between receptor agonism is rarely achieved, some agents have partial selectivity.

α₁ agonist

Main article: Alpha-1 adrenergic receptor § agonist

α₁ agonist: stimulates phospholipase C activity. (vasoconstriction and mydriasis; used as vasopressors, nasal decongestants and eye exams). Selected examples are:

• Methoxamine
• Methylnorepinephrine
• Midodrine
• Oxymetazoline
• Metaraminol
• Phenylephrine

α₂ agonist

Main article: Alpha-2 adrenergic receptor § Agonist

α₂ agonist: inhibits adenylyl cyclase activity, reduces brainstem vasomotor center-mediated CNS activation; used as antihypertensive, sedative & treatment of opiate dependence and alcohol withdrawal symptoms). Selected examples are:

• Clonidine (mixed alpha2-adrenergic and imidazoline-I1 receptor agonist)
• Guanfacine, (preference for alpha2A-subtype of adrenoceptor)
• Guanabenz (most selective agonist for alpha2-adrenergic as opposed to imidazoline-I1)
• Guanoxabenz (metabolite of guanabenz)
• Guanethidine (peripheral alpha2-receptor agonist)
• Xylazine,
• Tizanidine
• Methyldopa
• Fadolmidine
• Dexmedetomidine

Undetermined/unsorted

The following agents are also listed as agonists by MeSH.

• amidephrine
• amitraz
• anisodamine
• apraclonidine
• brimonidine
• cirazoline
• detomidine
• dexmedetomidine
• epinephrine
• ergotamine
• etilefrine
• indanidine
• lofexidine
• medetomidine
• mephentermine
• metaraminol
• methoxamine
• mivazerol
• naphazoline
• norepinephrine
• norfenefrine
• octopamine
• oxymetazoline
• phenylpropanolamine
• rilmenidine
• romifidine
• synephrine
• talipexole

Clinical significance

Alpha-adrenergic agonists are used in the treatment of glaucoma by decreasing the production of aqueous fluid by the ciliary bodies of the eye and also by increasing uveoscleral outflow.

See also

• Alpha blocker

References

External links

• Adrenergic alpha-Agonists at the US National Library of Medicine Medical Subject Headings (MeSH)

UpToDate Contents

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• 1. 昇圧剤および強心剤の使用 use of vasopressors and inotropes
• 2. 小児および思春期における注意欠陥多動性障害治療薬の薬理学 pharmacology of drugs used to treat attention deficit hyperactivity disorder in children and adolescents
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• 5. 横紋筋融解症の原因 causes of rhabdomyolysis

English Journal

• Trials in adult critical care that show increased mortality of the new intervention: Inevitable or preventable mishaps?

• Russell JA1,2, Williams MD3.
• Annals of intensive care.Ann Intensive Care.2016 Dec;6(1):17. doi: 10.1186/s13613-016-0120-1. Epub 2016 Feb 24.
• Several promising therapies assessed in the adult critically ill in large, multicenter randomized controlled trials (RCTs) were associated with significantly increased mortality in the intervention arms. Our hypothesis was that there would be wide ranges in sponsorship (industry or not), type(s) of
• PMID 26909519

• Mirtazapine prevents induction and expression of cocaine-induced behavioral sensitization in rats.

• Salazar-Juárez A1, Barbosa-Méndez S1, Jurado N1, Hernández-Miramontes R1, Leff P1, Antón B2.
• Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2016 Jul 4;68:15-24. doi: 10.1016/j.pnpbp.2016.02.010. Epub 2016 Feb 26.
• Cocaine abuse is a major health problem worldwide. Treatment based on both 5-HT2A/C and 5-HT3 receptor antagonists attenuate not only the effects of cocaine abuse but also the incentive/motivational effect related to cocaine-paired cues. Mirtazapine, an antagonist of postsynaptic α2-adrenergic, 5-H
• PMID 26922897

• Transfer of SAR information from hypotensive indazole to indole derivatives acting at α-adrenergic receptors: In vitro and in vivo studies.

• Sączewski J1, Hudson A2, Scheinin M3, Wasilewska A4, Sączewski F4, Rybczyńska A5, Ferdousi M2, Laurila JM3, Boblewski K5, Lehmann A5, Watts H6, Ma D6.
• European journal of medicinal chemistry.Eur J Med Chem.2016 Jun 10;115:406-15. doi: 10.1016/j.ejmech.2016.03.026. Epub 2016 Mar 14.
• In a search for novel antihypertensive drugs we applied scaffold hopping from the previously described α1-adrenergic receptor antagonists, 1-[(imidazolin-2-yl)methyl]indazoles. The aim was to investigate whether the α-adrenergic properties of the indazole core were transferable to the indole core.
• PMID 27031216

Japanese Journal

• 点鼻用血管収縮薬による薬剤性鼻閉33例の検討

• アレルギー 62(12), 1623-1630, 2013-12-30
• NAID 110009686158

• Beta-, Not Alpha-Adrenergic Stimulation Enhances Conduction Velocity in Cultures of Neonatal Cardiomyocytes

• Circulation journal : official journal of the Japanese Circulation Society 71(6), 973-981, 2007-05-20
• NAID 110006273843

• 除脳イヌの反射性排尿におけるα-アドレナリン作働性機構に関する研究

• 日本泌尿器科學會雜誌 84(4), 711-719, 1993-04-20
• NAID 110003086902

Related Links

• Alpha-adrenergic agonist | definition of alpha-adrenergic ...

alpha-adrenergic agonist An agent that selectively binds and activates alpha-adrenergic receptors. In the eye it causes mydriasis and reduces the production of aqueous humour. It is used topically in the treatment of glaucoma.

• Alpha-2 adrenergic receptor agonist | definition of alpha-2 ...

Alpha-2 agonist (alpha-2 adrenergic receptor agonist) A class of drugs that bind to and stimulate alpha-2 adrenergic receptors, causing responses similar to those of adrenaline and noradrenaline. They inhibit aqueous humor ...

Related Pictures

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★リンクテーブル★

リンク元	「αアドレナリン作動薬」「αアドレナリン刺激薬」「αアドレナリン受容体刺激薬」
関連記事	「adrenergic agonist」「adrenergics」「adrenergic」「alpha」

「αアドレナリン作動薬」

　　[★]

英

alpha-adrenergic agonist

関

αアドレナリン受容体刺激薬、αアドレナリン刺激薬

「αアドレナリン刺激薬」

　　[★]

英

alpha-adrenergic agonist

関

αアドレナリン作動薬、αアドレナリン受容体刺激薬

「αアドレナリン受容体刺激薬」

　　[★]

英

alpha-adrenergic agonist

関

αアドレナリン作動薬、α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

「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

　 　

「alpha」

　　[★]

α、アルファ

関

alfa