ライフサイエンスコーパス: pregnanolone

1 GABA(A) receptor agonists pentobarbital and pregnanolone.

2 mbinant receptors to the endogenous steroid, pregnanolone.

3 of 11- and 12-substituted derivatives of 5xi-pregnanolone (3alpha-hydroxy-5alpha-pregnan-20-one and 3

4 ed the actions of a carboxylated analogue of pregnanolone ((3alpha,5beta)-20-oxopregnane-3-carboxylic

5 n contrast, 5beta-pregnane-3alpha-ol-20-one (pregnanolone), 5beta-pregnane-3, 20-dione (5beta-dihydro

6 photolabeling reagent, (3alpha,5beta)-6-azi-pregnanolone (6-AziP), was used to photolabel membranes

7 o pairs of enantiomers (pregnanolone and ent-pregnanolone, allopregnanolone and ent-allopregnanolone)

8 We have used two pairs of enantiomers (pregnanolone and ent-pregnanolone, allopregnanolone and

9 n receptor activation by GABA, propofol, and pregnanolone and that beta2(Q185) participates in hydrop

10 es, whereas 5beta-pregnane-3alpha-ol-20-one (pregnanolone) and 5beta-dihydroprogesterone (5beta-DHP)

11 ate, dehydroepiandrosterone sulfate (DHEAS), pregnanolone, and allopregnanolone, modulate ionotropic

12 5beta-DHP reduction yielded the neurosteroid pregnanolone as the only product.

13 For synthetic pregnanolone derivatives substituted with a carboxylic a

14 on of 2.5 micrograms of the 3 beta-epimer of pregnanolone did not affect behavior in the plus-maze; a

15 Chronic exposure to pregnanolone, GABA, flurazepam or pentobarbital induces

16 In behavioral tests, pregnanolone hemipimelate showed neuroprotective activit

17 The steroid with the longest substituent, pregnanolone hemipimelate, had no effect on phasically a

18 el synthetic analog of pregnanolone sulfate, pregnanolone hemipimelate, inhibits tonic NMDAR currents

19 shock probe was not affected by any dose of pregnanolone in either intracranial site of injection.

20 maze was found after 2.5 and 5 micrograms of pregnanolone in the hippocampus, but not in the lateral

21 In addition, the EC50 for pregnanolone-induced homologous uncoupling (1.7 microM)

22 as decreased by 0.5, 2.5 and 5 micrograms of pregnanolone injection in the dorsal hippocampus or late

23 Moreover, heterologous uncoupling by pregnanolone is inhibited by the GABA site antagonist SR

24 t SR-95531, whereas homologous uncoupling by pregnanolone is resistant to SR-95531.

25 f the NR2A subunit on efficacy or potency of pregnanolone (or epipregnanolone) sulfate as an inhibito

26 with 3 alpha-hydroxy-5 beta-pregnan-20-one (pregnanolone), pentobarbital, flurazepam, or GABA, then

27 allopregnanolone (r(22)=-0.43, p=0.036) and pregNANolone (r(22)=-0.48, p=0.019) levels.

28 Dependent on the mutation, pregnanolone remained an inhibitor, transformed into a p

29 he percent direct activation by propofol and pregnanolone, respectively.

30 hibition of the hippocampus, mediated by the pregnanolone's action at the GABAA receptor, produces a

31 ents than the known endogenous neurosteroid, pregnanolone sulfate (IC50 = 24.6 muM).

32 muM) than the known endogeneous neurosteroid-pregnanolone sulfate (IC50 = 24.6 muM).

33 Pregnanolone sulfate (PAS) is an endogenous neurosteroid

34 ppocampal microisland cultures, we show that pregnanolone sulfate inhibits NMDAR currents induced by

35 ere, we show that an endogenous neurosteroid pregnanolone sulfate is more potent at inhibiting tonica

36 the mechanism of NMDA receptor inhibition by pregnanolone sulfate we used kinetic analyses of equilib

37 pregnanolone, tetrahydrodeoxycorticosterone, pregnanolone sulfate, allopregnanolone sulfate, and beta

38 a synthetic homologue of naturally occurring pregnanolone sulfate, inhibits NMDA-induced currents and

39 , we report that a novel synthetic analog of pregnanolone sulfate, pregnanolone hemipimelate, inhibit

40 compounds, including endogenous neurosteroid pregnanolone sulfate.

41 elected representatives of the three groups (pregnanolone, tetrahydrodeoxycorticosterone, pregnanolon

42 to potentiate (allopregnanolone) or inhibit (pregnanolone) the rho1 receptor is enantioselective.

43 aseptal injection of 2.5 and 5 micrograms of pregnanolone; the duration of burying behavior was decre

44 utations affected the ability of propofol or pregnanolone to potentiate a submaximal GABA response, b

45 tic propofol and the endogenous neurosteroid pregnanolone using whole cell macroscopic recordings.

46 intrahippocampal or intraseptal injection of pregnanolone were blocked by intracranial pretreatment w

47 The (+)-ACN enantiomer, (-)-ACN, and pregnanolone were somewhat less effective at inhibiting

48 e steroid, 3 alpha-OH-5 beta-pregnan-20-one (pregnanolone), were determined after injection into the