solubility
aqueous base: moderately soluble (Solutions should be stored at 4 °C.), ethanol: moderately soluble (Solutions should be stored at 4 °C.), H2O: slightly soluble
InChI
1S/C13H12N4O2/c1-16-11-9(12(18)17(2)13(16)19)14-10(15-11)8-6-4-3-5-7-8/h3-7H,1-2H3,(H,14,15)
SMILES string
CN1C(=O)N(C)c2nc([nH]c2C1=O)-c3ccccc3
InChI key
PJFMAVHETLRJHJ-UHFFFAOYSA-N
form
crystalline
potency
86 nM Ki for A1 receptors
color
off-white to light yellow
mp
>300 °C (lit.)
Gene Information
human ... ADORA1(134), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316)
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Biochem/physiol Actions
Selective A1 adenosine receptor antagonist.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
W R Ezzat et al.
The American journal of physiology, 252(4 Pt 2), H836-H845 (1987-04-01)
Pressure-flow autoregulation, although weak, was seen in the hepatic artery (HA) of every cat that also showed dilation to infused adenosine. Several means of quantitating autoregulation are described and evaluated, and all indices showed that the selective adenosine antagonists, 8-phenyltheophylline
J Sawynok et al.
Neuropharmacology, 30(8), 871-877 (1991-08-01)
Morphine was injected into the periaqueductal gray region of the rat and 8-phenyltheophylline, an adenosine receptor antagonist, was injected intrathecally 15 or 30 min later, to determine whether supraspinally-administered morphine activated descending mechanisms to release adenosine (or a nucleotide which
Daphne Merkus et al.
American journal of physiology. Heart and circulatory physiology, 285(1), H424-H433 (2003-03-15)
In dogs, only combined blockade of vasodilator pathways [via adenosine receptors, nitric oxide synthase (NOS) and ATP-sensitive K+ (KATP) channels] results in impairment of metabolic vasodilation, which suggests a redundancy design of coronary flow regulation. Conversely, in swine and humans
Ana Rita Pinheiro et al.
Cell communication and signaling : CCS, 11, 70-70 (2013-09-21)
Chronic musculoskeletal pain involves connective tissue remodeling triggered by inflammatory mediators, such as bradykinin. Fibroblast cells signaling involve changes in intracellular Ca2+ ([Ca2+]i). ATP has been related to connective tissue mechanotransduction, remodeling and chronic inflammatory pain, via P2 purinoceptors activation.
Gregory M Dick et al.
American journal of physiology. Heart and circulatory physiology, 294(5), H2371-H2381 (2008-04-01)
We previously demonstrated a role for voltage-dependent K(+) (K(V)) channels in coronary vasodilation elicited by myocardial metabolism and exogenous H(2)O(2), as responses were attenuated by the K(V) channel blocker 4-aminopyridine (4-AP). Here we tested the hypothesis that K(V) channels participate
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