TPMPA (hydrate)

TPMPA is a GABAA-rho1 (rho1 GABAC) receptor antagonist that is 8-fold selective for GABAA-rho1 over GABAA-rho2 (rho2 GABAC) receptors expressed in X. laevis oocytes (Kbs = 2 and 16 µM, respectively). In rat hippocampal slices, TPMPA blocks the inhibitory effect of the GABAB agonist 3-APMPA on excitatory postsynaptic currents (EPSCs) with an EC50 value of 490 µM. TPMPA (100 µM) increases light sensitivity and the maximal response of rat retinal ganglion cells without altering their dynamic range. In sleeping rats, TPMPA (50 µg, i.c.v.) increases waking from 45 to 62% compared to a vehicle control and decreases slow-wave and paradoxical sleep (REM) by 11 and 5.4%, respectively.Formal Name: P-methyl-P-(1,2,3,6-tetrahydro-4-pyridinyl)-phosphinic acid, hydrate. Molecular Formula: C6H12NO2P . XH2O. Formula Weight: 161.1. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: PBS (pH 7.2): 10 mg/ml. SMILES: CP(C1=CCNCC1)(O)=O.O. InChi Code: InChI=1S/C6H12NO2P.H2O/c1-10(8,9)6-2-4-7-5-3-6,/h2,7H,3-5H2,1H3,(H,8,9),1H2. InChi Key: GXVWAQPRAQORGS-UHFFFAOYSA-N.