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1 xy-5alpha-pregnan-20-one (3alpha,5alpha-THP; allopregnanolone).
2 ely catalyzes the intracellular oxidation of allopregnanolone.
3 to synthesize 5alpha-dihydroprogesterone and allopregnanolone.
4 re observed for estradiol, progesterone, and allopregnanolone.
5 nol, t-butanol, pentobarbital, diazepam, and allopregnanolone.
6 e modulator DHEAS and the positive modulator allopregnanolone.
7 s were markedly prolonged in the presence of allopregnanolone.
8 mplicated in the etiology of PMDD, including allopregnanolone.
9 eous formulation of the neuroactive steroid, allopregnanolone.
10 tor finasteride, as well as progesterone and allopregnanolone.
11 ersion of progesterone into the neurosteroid allopregnanolone.
12 the presence of transmitter and the steroid allopregnanolone.
13 s including sensitivity to the neurosteroid, allopregnanolone.
14 with EC50 values similar to those found for allopregnanolone.
15 (2-minute) application of GABA or GABA plus allopregnanolone.
16 r a combination of clonazepam with exogenous allopregnanolone.
17 Finally, PPI deficits were exacerbated by allopregnanolone (10 mg/kg, IP) and attenuated by proges
19 um, cultures were exposed to DHEA, DHEAS, or allopregnanolone (10(-10), 10(-8), or 10(-6) M), or vehi
20 -(trifluoromethyl)-3H-diazirine-3-yl)benzoxy]allopregnanolone ([(3)H]21-pTFDBzox-AP), a potent GABA(A
22 that the neuroactive progesterone metabolite allopregnanolone (3alpha-hydroxy-5alpha-pregnan-20-one)
25 e mutations could not confer potentiation by allopregnanolone (3alpha5alphaP) when expressed in recep
26 ceptor modulation by the endogenous steroids allopregnanolone (3alpha5alphaP), pregnenolone sulfate,
29 quantitative method for the determination of allopregnanolone (5alpha,3alpha-THP) and related neurost
31 ress) and induces peripheral biosynthesis of allopregnanolone, a gamma-aminobutyric acidergic neurost
32 ulates opioid production in the brainstem is allopregnanolone, a neurosteroid metabolite of progester
33 r levels of progesterone and lower levels of allopregnanolone, a neurosteroid metabolite of progester
34 47 injection), an intravenous formulation of allopregnanolone, a positive allosteric modulator of gam
35 yl-3-hydroxybutyryl-CoA and the oxidation of allopregnanolone, a positive modulator of the gamma-amin
36 d and unsulfated steroids, such as DHEAS and allopregnanolone, act at distinct sites implies that ste
40 3alpha-hydroxysteroid-5alpha-pregnan-20-one (allopregnanolone) acts as a positive allosteric modulato
44 ct of acute ethanol administration and acute allopregnanolone administration on spontaneous hippocamp
45 ult mice previously stressed during puberty, allopregnanolone administration was sufficient to reprod
50 gression associated with a decrease of brain allopregnanolone (Allo) content and a decrease (approxim
52 ctase type I (5alpha-RI) mRNA expression and allopregnanolone (Allo) levels in selected neurons of th
54 ogesterone (P4), and the neuroactive steroid allopregnanolone (ALLO) may disrupt the molecular mechan
56 systemic administration of the neurosteroid allopregnanolone (ALLO), a positive allosteric modulator
58 (plKO), we investigate how reduced placental allopregnanolone (ALLO), an anti-inflammatory neurostero
61 ments, such as the neuroactive steroid (NAS) allopregnanolone (AlloP, brexanolone), may induce autoph
64 -AP), a general anesthetic and photoreactive allopregnanolone analog that is a potent GABA(A)R PAM, t
66 e Food and Drug Administration's approval of allopregnanolone analogs, which function as positive all
67 ssant effects of exogenous administration of allopregnanolone analogs; yet, the role of endogenous al
69 rosteroids can reduce HPA axis responses, so allopregnanolone and 3beta-androstanediol (3beta-diol; 5
70 d 5alpha-DHP reduction yielded two products, allopregnanolone and 5alpha,20alpha-tetrahydroprogestero
71 positive allosteric modulators of GABA(A)Rs allopregnanolone and DS2 also induced larger current shi
72 ntiomers (pregnanolone and ent-pregnanolone, allopregnanolone and ent-allopregnanolone) and show that
74 pregnenolone following a swim stress and for allopregnanolone and epiallopregnanolone following allop
75 sults further demonstrate similar effects of allopregnanolone and ethanol on hippocampal neurophysiol
76 [(3)H]flunitrazepam as radioligand in which allopregnanolone and its active analogues stimulated the
79 azepam had recognizable common features with allopregnanolone and pentobarbital but was also distinct
81 001) were observed in the frontal cortex for allopregnanolone and pregnenolone following a swim stres
82 imol binding in the presence of the steroids allopregnanolone and pregnenolone sulfate, although the
84 e modulated by the endogenous neurosteroids, allopregnanolone and tetrahydro-deoxycorticosterone.
85 ride, indicating a causal connection between allopregnanolone and the endogenous opioid mechanism.
86 uency and amplitude of sIPSCs, the action of allopregnanolone and the hypertrophy of oxytocin neurone
87 in the presence of the potentiating steroid allopregnanolone and the inhibitory steroid pregnenolone
89 ures of a synaptic GABA(A) receptor bound to allopregnanolone and two inhibitory sulfated neurosteroi
90 of combinations of GABA, taurine, propofol, allopregnanolone and/or the inhibitory steroid pregnenol
91 d ent-pregnanolone, allopregnanolone and ent-allopregnanolone) and show that the ability to potentiat
92 one, a progesterone metabolite also known as allopregnanolone, and 5alpha-androstane-3alpha,17beta-di
93 ositive allosteric modulators clonazepam and allopregnanolone, and by the NMDA receptor antagonists d
94 ); the GABA(A) receptor modulators diazepam, allopregnanolone, and Ro15-4513; and the L-type Ca2+ cha
96 BA, propofol, pentobarbital, and the steroid allopregnanolone, and the observed steady-state response
97 TS-associated responses via the neurosteroid allopregnanolone (AP) in an animal model of repetitive b
98 ated that the progesterone (PROG) metabolite allopregnanolone (AP) is more potent than PROG in the tr
108 strogen and progesterone, and its metabolite allopregnanolone, are anti-inflammatory, reshape compete
111 that a single injection of the neurosteroid allopregnanolone at postnatal day 7 significantly prolon
114 increased in pregnant mice in the absence of allopregnanolone attributable to brain region-specific d
116 a clinical neurosteroid general anesthetic, allopregnanolone, believed to occupy the colchicine site
117 s of certain bacterial progestins, including allopregnanolone, better known as brexanolone, an FDA-ap
118 In contrast, both allopregnanolone and epi-allopregnanolone bind to intrasubunit sites in the beta(
120 one, but not its inhibitory 3beta-epimer epi-allopregnanolone, binds to the canonical beta(3)(+)-alph
122 oprogesterone (5alpha-DHP), the last step in allopregnanolone biosynthesis, is catalyzed by 3alpha-hy
123 ion of allopregnanolone reduces anxiety, and allopregnanolone blockade impairs social and affective f
124 m-effects meta-analysis of studies comparing allopregnanolone blood concentrations in women with vers
125 herapy (NRT) with GABA-A receptor-modulating allopregnanolone (brexanolone) shows promise as the firs
126 We found that the potentiating neurosteroid, allopregnanolone, but not its inhibitory 3beta-epimer ep
127 conversion of 5alpha-dihydroprogesterone to allopregnanolone by human 3alpha-HSD type III 10- to 30-
129 so have membrane actions, and in particular, allopregnanolone can act at GABAA receptors to potentiat
130 ty of GABA(A) receptors of epileptic DGCs to allopregnanolone can increase susceptibility to seizures
136 and certain other small molecules increased allopregnanolone concentrations in vivo by activating 3a
137 siological and pharmacological modulation of allopregnanolone concentrations in vivo have been extens
141 microbiota or metabolites influences central allopregnanolone content after trafficking to the brain,
142 lpha expression downregulation and decreased allopregnanolone content and ameliorates depressive-like
144 und that at comparable doses, the effects of allopregnanolone, despite purported selectivity for cert
148 eptors, we still do not fully understand how allopregnanolone exerts persistent antidepressant effect
149 we used 11beta-(p-azidotetrafluorobenzoyloxy)allopregnanolone (F(4)N(3)Bzoxy-AP), a general anestheti
150 teroid 3alpha-hydroxy-5alpha-pregnan-20-one (allopregnanolone) facilitates GABA(A) receptor-mediated
152 racterize the role of 3alpha-HSD type III in allopregnanolone formation and suggest that activation o
155 eparate a rapid antidepressant neurosteroid, allopregnanolone, from other GABA(A) positive modulators
156 ing baseline noise in DGCs were sensitive to allopregnanolone, furosemide, and loreclezole and insens
159 )3-hydroxypregnan-20-one (3alpha,5alpha-THP, allopregnanolone) has protective activity in animal mode
160 s of progesterone and its natural metabolite allopregnanolone have been synthesized and screened usin
163 bitors (SSRIs) could alter concentrations of allopregnanolone in human cerebral spinal fluid and in r
165 metabolites pregnenolone sulfate (PregS) and allopregnanolone in serum are inversely associated with
169 anolone analogs; yet, the role of endogenous allopregnanolone in the pathophysiology of depression re
170 progesterone to its neurosteroid metabolite allopregnanolone in women with premenstrual dysphoric di
171 ypothesis, the current data demonstrate that allopregnanolone, in a dose-dependent manner, induces a
172 ones and NASs, particularly progesterone and allopregnanolone, in preparing the brain for the transit
173 s derivatives 5alpha-dihydroprogesterone and allopregnanolone, in the prefrontal cortex (PFC) of D1CT
174 utic potential of a neurogenic neurosteroid, allopregnanolone, in the restoration of the components o
176 CR and Western blot validation revealed that allopregnanolone increased the expression of genes that
178 om the isolated supraoptic nucleus, but only allopregnanolone induced significant release of vasopres
181 ntrast, in supraoptic nuclei from adult rats allopregnanolone-induced oxytocin release was much small
184 nifedipine, consistent with the finding that allopregnanolone induces a rapid increase in intracellul
186 that the neuroactive progesterone metabolite allopregnanolone induces these changes in HPA responsive
193 ions are associated with postpartum RSFC and allopregnanolone is associated with postpartum intra-DMP
195 -hydroxypregnan-20-one (3alpha,5alpha-THP or allopregnanolone) is a positive modulator of GABAA recep
196 eroid 3alpha-hydroxy-5alpha-pregnane-20-one (allopregnanolone) is a potent endogenous modulator of GA
197 ositive allosteric modulators; one of these, allopregnanolone, is the only drug approved specifically
198 n non-classical progesterone actions through allopregnanolone, its neuroactive steroid metabolite, an
201 e, symptom cyclicity maintained), and plasma allopregnanolone levels increased in women with PMDD fro
207 s provide initial neuroimaging evidence that allopregnanolone may be a target for pharmacologic inter
210 ted by 5alpha-reductase, and by reduction to allopregnanolone, mediated by 3alpha-hydroxysteroid dehy
211 ntly, the acute addition of the neurosteroid allopregnanolone mitigated functional impairments observ
212 rosterone sulfate (DHEAS), pregnanolone, and allopregnanolone, modulate ionotropic amino acid neurotr
213 , larger in amplitude, and less sensitive to allopregnanolone modulation than those recorded from DGC
215 d subcutaneously (0.2 ml) with either 3mg/kg allopregnanolone or 20% w/v beta-cyclodextrin vehicle.
217 ne) and show that the ability to potentiate (allopregnanolone) or inhibit (pregnanolone) the rho1 rec
218 ract with distinct sites and either enhance (allopregnanolone) or reduce (pregnenolone sulfate) recep
219 r association to the change in estradiol and allopregnanolone over the course of pregnancy, suggestin
220 ibition studies for 5alpha-DHP reduction and allopregnanolone oxidation indicated that 3alpha-HSD typ
223 anol on hippocampal neurophysiology and that allopregnanolone plays a key role in producing ethanol-i
224 -3-hydroxypregnan-20-one (3alpha,5alpha-THP, allopregnanolone)-positive cells in the VTA, but did not
225 lone), and 5alpha-pregnane-3alpha-ol-20-one (allopregnanolone) potentiated the GABA-evoked currents f
226 ectrophysiology support a mechanism by which allopregnanolone potentiates channel activity and sugges
228 ment with a negative allosteric modulator of allopregnanolone promoted avoidance behavior in control
230 e HRSA correlated negatively with changes in allopregnanolone (r(22)=-0.43, p=0.036) and pregNANolone
232 trate that in response to emotional stimuli, allopregnanolone reduces activity in regions associated
234 ABA site are potentiated by the neurosteroid allopregnanolone regardless of whether the steroid inter
236 ute treatment (once/week for two weeks) with allopregnanolone restored the number of tyrosine hydroxy
237 from pregnant mice compared with virgin, but allopregnanolone reverted the threshold for inducing epi
240 ed sensitivity to Zn2+ indicate that loss of allopregnanolone sensitivity is likely to be due to alte
242 alogs with molecular pharmacology similar to allopregnanolone (SGE-516 [tool compound] and zuranolone
243 s suggest that altered vHIP progesterone and allopregnanolone signaling during diestrus increases avo
246 rodeoxycorticosterone, pregnanolone sulfate, allopregnanolone sulfate, and beta-estradiol) and probed
247 ress may exacerbate TS symptoms by promoting allopregnanolone synthesis in the PFC, and corroborate p
248 ockdown of rate-limiting enzymes involved in allopregnanolone synthesis, 5alpha-reductase type 1 and
251 regnancy, inhibition of 5alpha-reductase (an allopregnanolone-synthesizing enzyme) with finasteride r
253 rtle was probably mediated by its metabolite allopregnanolone [tetrahydroprogesterone (THP)], because
254 e, converting 3alpha-tetrahydroprogesterone (allopregnanolone) to dihydroprogesterone and 3alpha-andr
258 aken together, our results clearly show that allopregnanolone treatment not only reduces cholesterol
259 Here, we further characterized the effect of allopregnanolone treatment on cholesterol accumulation,
262 (mediated by neuroactive metabolites such as allopregnanolone), typified by irritability and hyperaro
263 lity that are restored by the high levels of allopregnanolone under normal conditions but under patho
264 endogenous oxytocin, and (ii) the effect of allopregnanolone upon oxytocin release changes with age,
266 the adult, oxytocin effects are modulated by allopregnanolone via an interaction with inhibitory GABA
268 s also noted that MPTP treated mice to which allopregnanolone was administered had an increase in Brd
271 tivity to the locomotor stimulant effects of allopregnanolone was determined in 24 BXD recombinant in
275 We hypothesized that the pregnancy hormone, allopregnanolone, was involved in presentation of the bl
276 5alpha-reduced neurosteroids, predominantly allopregnanolone, we found that immunostaining in the CA
277 g GABA(A) receptors and endogenous levels of allopregnanolone were reduced in the BLA following CUS.
278 anesthetic steroids such as alphaxalone and allopregnanolone, which have a 5alpha-configuration at t
279 amide, chlorthalidone, and the neurosteroid, allopregnanolone, which inhibits chloride transport, pro
280 s of the weight spectrum have low mean serum allopregnanolone, which is associated with increased dep
281 Cs is significantly longer in the absence of allopregnanolone, which now has no significant effect.
282 the combination of GABA and the neurosteroid allopregnanolone, which was intended to desensitize a fr