3-Aminopropylphosphonic Acid是与膦酸的磷相连的氢被3-氨基丙基取代的膦酸,是GABAB受体(GABABR)的部分激动剂和基础催乳素分泌拮抗剂。
产品描述
3-aminopropylphosphonic acid (3-APPA) is a phosphonic analog of GABA that acts as a partial agonist of GABAB receptors (IC50 = 1.5 μM in a radioligand binding assay).
体外活性
3-aminopropylphosphonic acid (IC50 1.5 microM) and 4-aminobutyl-phosphonic acid (IC50 3.9 μM) were much more potent than anticipated from their relatively weak GABAB antagonist actions [1]. 3-aminopropylphosphonic acid was a potent inhibitor (IC50 6μM) of the binding of [3H]GABA to rat brain membranes under GABAB conditions, i.e. in the presence of 0.1 mM isoguvacine and displaceable by 0.1 mM (+)-baclofen [1].
体内活性
3-aminopropylphosphonic acid induces relaxation in unstimulated isolated guinea pig ileum longitudinal muscle and reverses GABA- and baclofen-induced inhibition of twitch responses in isolated guinea pig ileum longitudinal muscle. 3-APPA (5 mg/kg) completely inhibits GABA- and baclofen-induced inhibition of vagally stimulated bronchospasms in guinea pigs. It also reverses the antitussive effect of baclofen in cats when administered at a dose of 3 mg/kg.
Cas No.
13138-33-5
分子式
C3H10NO3P
分子量
139.09
储存和溶解度
Ethanol:PBS (pH 7.2) (1:3):0.25 mg/mL
DMF:5 mg/mL
DMSO:2 mg/mL
Ethanol:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years