化驗
≥98% (HPLC)
形狀
powder
顏色
off-white
溶解度
H2O: >5 mg/mL
起源
Abbott
儲存溫度
2-8°C
SMILES 字串
O.Br.CS(=O)(=O)Nc1c(O)ccc2C(CCCc12)C3=NCCN3
InChI
1S/C14H19N3O3S.BrH.H2O/c1-21(19,20)17-13-10-3-2-4-11(14-15-7-8-16-14)9(10)5-6-12(13)18;;/h5-6,11,17-18H,2-4,7-8H2,1H3,(H,15,16);1H;1H2
InChI 密鑰
PRYXREGSOWDDDR-UHFFFAOYSA-N
應用
A-61603 is an α1A agonist and has been studied to understand the functional roles of α(1)-adrenoceptor subtypes in mouse carotid arteries. A-61603 stimulated phosphoinositide hydrolysis In fibroblast cells transfected with α1a receptors.
生化／生理作用
A-61603 is an α1A agonist. In radioligand binding assays, A-61603 was at least 35-fold more potent at α1A receptors than at α1b or α1d sites. In fibroblast cells transfected with α1a receptors, A-61603 more potently stimulated phosphoinositide hydrolysis than norepinephrine, and was antagonized by prazosin. A-61603 is less potent in cells transfected with α1b or α1d receptors. It is a potent agonist at α1A receptors in rat vas deferens (200- to 300-fold more potent than norepinephrine or phenylephrine, respectively) and in isolated canine prostate strips (130- to 165-fold more potent than norepinephrine or phenylephrine, respectively). In contrast, it is only 40-fold more potent than phenylephrine at α1B sites in rat spleen and 35-fold less potent at rat aortic, α1D sites. A-61603 induces a pressor response in conscious rats at doses 50- to 100-fold lower than phenylephrine.
特點和優勢
This compound is featured on the α1-Adrenoceptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
訊號詞
Warning
危險聲明
危險分類
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
標靶器官
Respiratory system
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
Clare Deighan et al.
British journal of pharmacology, 144(4), 558-565 (2005-01-19)
1. alpha(1)-Adrenoceptor (AR) subtypes in mouse carotid arteries were characterised using a combination of agonist/antagonist pharmacology and knockout (KO) mice. 2. Phenylephrine (PE) was most potent in the alpha(1B)-KO (pEC(50)=6.9+/-0.2) followed by control (pEC(50)=6.3+/-0.06) and alpha(1D)-KO (pEC(50)=5.5+/-0.07). Both N-[5-(4,5-dihydro-1H-imidazol-2yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl] methanesulphonamide
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