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Merck
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重要文件

A9611

Sigma-Aldrich

Atipamezole

≥98% (HPLC)

同義詞:

4-(2-Ethyl-2,3-dihydro-1H-inden-2-yl)-1H-Imidazole, Antisedan, MPV 1248

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About This Item

經驗公式(希爾表示法):
C14H16N2
CAS號碼:
分子量::
212.29
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
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化驗

≥98% (HPLC)

形狀

powder

顏色

white to brown

溶解度

DMSO: ≥30 mg/mL

儲存溫度

room temp

SMILES 字串

CCC1(Cc2ccccc2C1)c3c[nH]cn3

InChI

1S/C14H16N2/c1-2-14(13-9-15-10-16-13)7-11-5-3-4-6-12(11)8-14/h3-6,9-10H,2,7-8H2,1H3,(H,15,16)

InChI 密鑰

HSWPZIDYAHLZDD-UHFFFAOYSA-N

一般說明

Atipamezole has an imidazole structure and gets localized in the central nervous system on administration.[1]

應用

Atipamezole has been used as a α2-adrenoceptor antagonist in mesencephalic trigeminal nucleus (MTN) neurons,[2] CD4+ T-lymphocyte[3] and human embryonic kidney (HEK293) membrane preparation.[4]

生化/生理作用

Atipamezole elicits affinity towards adrenoreceptor subtypes namely α2A, α2B and α2C. High levels of atipamezole impairs cognitive functions. It also reverses the adrenoreceptor agonist functionalities.[1] Atipamezole shows no affinity towards muscarinic[1] and dopamine or neurotransmitter receptors.[5] Atipamezole when used along with morphine elicits antinociceptive effects.[6]
Atipamezole is a selective α2 adrenergic blocker. Atipamezole is more potent than yohimbine; it is very selective for α2 adrenergic vs α1 sites, but not selelctive for α2 subtypes.
Atipamezole is a selective α2 adrenergic blocker; neutral antagonist

特點和優勢

This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the α2-Adrenoceptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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D Van Vynckt et al.
The Journal of small animal practice, 52(12), 638-644 (2011-10-25)
To assess the influence of two sedation protocols on the degree of lameness in dogs. Fifty lame dogs were allocated to one of two sedation protocols. Group ACPM (acepromazine + methadone; n=25) was sedated with acepromazine and methadone. Group MED
Tuomas O Lilius et al.
Anesthesia and analgesia, 114(6), 1353-1358 (2012-05-05)
Opioid analgesics are effective in the treatment of chronic pain, but they have serious adverse effects such as development of tolerance and dependence. Adrenergic α(2) agonists and μ-opioid receptor agonists show synergistic potentiation and cross-tolerance in spinal analgesia, whereas α(2)-adrenergic
Brian Milne et al.
Anesthesia and analgesia, 112(6), 1500-1503 (2011-05-06)
Ultralow-dose opioid antagonists prolong opioid antinociception and block tolerance. In this study we determined whether low doses of the α-2 adrenergic receptor (A2-R) antagonist, atipamezole, similarly influenced A2-R-induced antinociception and tolerance. In rats, intrathecal norepinephrine (NE) or clonidine in combination
Antti Pertovaara et al.
CNS drug reviews, 11(3), 273-288 (2006-01-04)
Atipamezole is an alpha2-adrenoceptor antagonist with an imidazole structure. Receptor binding studies indicate that its affinity for alpha2-adrenoceptors and its alpha2/alpha1 selectivity ratio are considerably higher than those of yohimbine, the prototype alpha2-adrenoceptor antagonist. Atipamezole is not selective for subtypes
The C-terminal half of the alpha 2C-adrenoceptor determines the receptor's membrane expression level and drug selectivity
Jahnsen JA and Uhlen S
Naunyn-Schmiedeberg'S Archives of Pharmacology, 386(12), 1031-1040 (2013)

文章

Learn about alpha-2 adrenoceptor and its subtypes, mediated responses, and applications of agonists. Included is a list of available products and a comparison table.

DISCOVER Bioactive Small Molecules for Neuroscience

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