3-APPA explained

Cas Number:103680-47-3
Unii:QMT5SS3QRE
Pubchem:121956
Iuphar Ligand:1081
Chemspiderid:10462431
Chembl:112203
Iupac Name:3-aminopropylphosphinic acid
C:3
H:10
N:1
O:2
P:1
Smiles:C(CN)CP(=O)O
Stdinchi:1S/C3H10NO2P/c4-2-1-3-7(5)6/h7H,1-4H2,(H,5,6)
Stdinchikey:ZTHNRNOOZGJLRR-UHFFFAOYSA-N

3-Aminopropylphosphinic acid, also known in the literature as 3-APPA or CGP 27492,[1] is a compound used in scientific research which acts as an agonist at the GABAB receptor. It is part of a class of phosphinic acid GABAB agonists,[2] which also includes SKF-97,541. It has a binding affinity (pKi) to the GABAB receptor of 8.30 (i.e., ~3 nM).[3]

Notes and References

  1. Web site: 3-APPA . IUPHAR/BPS Guide to Pharmacology . March 23, 2021.
  2. Lacey G, Curtis DR . Phosphinic acid derivatives as baclofen agonists and antagonists in the mammalian spinal cord: an in vivo study . Experimental Brain Research . 101 . 1 . 59–72 . 1994 . 7843303 . 10.1007/BF00243217 . 19055950 .
  3. Froestl W, Mickel SJ, von Sprecher G, Diel PJ, Hall RG, Maier L, Strub D, Melillo V, Baumann PA, Bernasconi R . 6 . Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists . Journal of Medicinal Chemistry . 38 . 17 . 3313–31 . August 1995 . 7650685 . 10.1021/jm00017a016 .