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 eroids, one each for the inhibitory steroids pregnanolone (3alpha5betaP), 3alpha5betaP sulfate, and b

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

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

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

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

10 in older and male adults, is associated with pregnanolone and progesterone-related sulfated metabolit

11 LECs metabolize progesterone to 6a-OH-pregnanolone and reactivate progesterone from a precurso

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

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

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

15 Allopregnanolone (3alpha5alpha-P), pregnanolone, and their synthetic derivatives are potent

16 5beta-DHP reduction yielded the neurosteroid pregnanolone as the only product.

17 For synthetic pregnanolone derivatives substituted with a carboxylic a

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

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

20 In behavioral tests, pregnanolone hemipimelate showed neuroprotective activit

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

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

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

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

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

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

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

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

29 Enhanced progesterone metabolism to 6a-OH-pregnanolone occurs in complicated pregnancies such as i

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

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

32 nd those with a one-unit increase in the log pregnanolone/progesterone ratio at T3 had lower odds (OR

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

34 unit increase in the log isoallopregnanolone/pregnanolone ratio at the third trimester (T3) had highe

35 with the C-20 carbonyl of 3alpha5alpha-P or pregnanolone reduced to a hydroxyl, binding affinity is

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

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

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

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

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

41 Pregnanolone sulfate (PAS) is an endogenous neurosteroid

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

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

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

45 butyric acid, 3-methylphenylacetic acid, and pregnanolone sulfate) and 6 were lower in women with GD

46 pregnanolone, tetrahydrodeoxycorticosterone, pregnanolone sulfate, allopregnanolone sulfate, and beta

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

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

49 compounds, including endogenous neurosteroid pregnanolone sulfate.

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

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

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

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

54 ry bile acid, and neuroactive glucocorticoid/pregnanolone-type steroidal metabolites.

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

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

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

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