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3-APPA(CGP 27492)(mM/ml)

Names

[ CAS No. ]:
103680-47-3

[ Name ]:
3-APPA(CGP 27492)(mM/ml)

[Synonym ]:
3-Aminopropanephosphinic acid
3-amnopropylphosphonous acid
3-Aminopropylphosphonous acid
Cgp 27 492

Biological Activity

[Description]:

3-Aminopropylphosphinic acid (3-APPA), a phosphonic analog of GABA, is a GABAB receptor agonist[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[In Vitro]

3-Aminopropylphosphinic acid (10 μM) causes a concentration-dependent inhibition of the cholinergic twitch contraction in the electrically stimulated ileum (IC50=1.84 + 0.23 μM), but does not produce an initial contraction[2].

[In Vivo]

3-Aminopropylphosphinic acid (5 mg/kg; iv) blocks the inhibitory effects of GABA against vagal broncho-spasm in guinea pigs[3]. Animal Model: guinea pigs[3] Dosage: 5 mg/kg Administration: IV Result: Blocked the inhibitory effects of GABA against vagal broncho-spasm.

[References]

[1]. [1]Luzzi S, Franchi-Micheli S, Ciuffi M, Pajani A, Zilletti L. GABA-related activities of amino phosphonic acids on guinea-pig ileum longitudinal muscle. J Auton Pharmacol. 1986 Sep;6(3):163-9.

[2]. [2]Hills JM, Dingsdale RA, Parsons ME, Dolle RE, Howson W. 3-Aminopropylphosphinic acid--a potent, selective GABAB receptor agonist in the guinea-pig ileum and rat anococcygeus muscle. Br J Pharmacol. 1989 Aug;97(4):1292-6.

[3]. [3]Chapman RW, Danko G, Rizzo C, Egan RW, Mauser PJ, Kreutner W. Prejunctional GABA-B inhibition of cholinergic, neurally-mediated airway contractions in guinea-pigs. Pulm Pharmacol. 1991;4(4):218-24.

Chemical & Physical Properties

[ Molecular Formula ]:
C3H10NO2P

[ Molecular Weight ]:
123.09

[ Exact Mass ]:
122.03700

[ PSA ]:
95.92000

[ Vapour Pressure ]:
0.001mmHg at 25°C

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds