erβ selective antagonist phtpp  (Tocris)

Journal: Brain research

Article Title: Estrogen receptor α regulates the IKKs/NF-kB activity involved in the development of mechanical allodynia induced by REM sleep deprivation in rats.

doi: 10.1016/j.brainres.2024.149269

Figure Lengend Snippet: Fig. 3. ERα but not ERβ regulates BMS-345541-prevented REMSD-induced allodynia in female rats. A) Effect of intrathecal injection of BMS-345541 pretreatment (preTx BMS 10 µg) in the establishment of mechanical allodynia induced by REM sleep deprivation (REMSD) for two days in intact female rats (F), female rats with vehicle (Veh), rats treated with ICI (ICI+preTx BMS), rats treated with a selective ERα antagonist (MPP+preTx BMS) or rats treated with a selective ERβ antagonist (PHTPP+preTx BMS). B) Area under the curve (AUC) obtained from time course in A. C) Effect of intrathecal injection of BMS-345541 pretreatment (preTx BMS 10 µg) in the establishment of mechanical allodynia induced by REMSD in female rats with vehicle (Veh), non-ovariectomized female rats (F), ovariectomized rats (OVX) and ovariectomized rats in the presence of ERα agonist (OVX+PPT). D) Area under the curve obtained from time course in C. Data are expressed as the mean ± SEM (n = 6). *** p < 0.001 versus Veh group; # # # p < 0.001 versus intact female rats with pretreatment (F) by one-way ANOVA followed by the Tukey test.

Article Snippet: PHTPP [4-[2-fenil-5,7-bis(trifluorometil) pirazolo[1,5-a]-pirimidin-3-il]fenol], a selective ERβ antagonist (Cat. No SC-204191, Santa Cruz Biotecnology, Dallas, TX) and PPT(1,3,5-Tris (4-hydroxyphenyl)-4-propyl-1H-pyrazole), a selective ERα agonist (Cat. No. SC-297946, Santa Cruz Biotechnology, Dallas, TX) were dissolved in 1 % DMSO in saline.

Techniques: Injection

Journal: eNeuro

Article Title: Local Synthesis of Estradiol in the Rostral Ventromedial Medulla Protects against Widespread Muscle Pain in Male Mice

doi: 10.1523/ENEURO.0332-24.2024

Figure Lengend Snippet: Pharmacological drugs utilized for RVM microinjection experiments

Article Snippet: PHTPP , ER-β antagonist , Tocris Bioscience , 2662 , 1 μM , 2% DMSO; 0.9% saline.

Techniques: Microinjection, Concentration Assay, Saline

Journal: Science Advances

Article Title: 27-Hydroxycholesterol acts on estrogen receptor α expressed by POMC neurons in the arcuate nucleus to modulate feeding behavior

doi: 10.1126/sciadv.adi4746

Figure Lengend Snippet: ( A to L ) Immunofluorescent staining for c-Fos (red) in the arcuate nucleus of the hypothalamus (ARH) of female [(A) to (F)] and male [(G) to (L)] ERα-ZsGreen mice 90 min after a single bolus ICV infusion of vehicle or 27HC (0.1 nmol). White arrows point to dual-colored neurons with ERα (green) and c-Fos (red) expressed. ( M and N ) Summary of quantification per section of female and male mice ( n = 3). ( O ) Schematic of POMC neurons in the ARH (POMC ARH ) treated with 27HC for electrophysiology recordings. ( P ) A micrographic image showing a recorded POMC ARH (red) neuron of male mice POMC-Cre/Rosa26-LSL-tdTOMATO mice. ( Q ) Resting membrane potential (RM) of POMC ARH neurons before and after 27HC treatment. ( R ) Summary of the responsive ratio of POMC ARH neurons for all doses of 27HC. ( S and T ) The effects of 100 nM 27HC on RM before and after ERα antagonist BHPI (S) or ERβ antagonist PHTPP (T) incubation. The brain slices were first preincubated with presynaptic inhibitors 1 μM TTX (a voltage-gated sodium channel blocker) + 30 μM CNQX (an AMPA receptor antagonist) + 30 μM DAP-5 (an NMDA receptor antagonist) + 50 μM bicuculline (a GABA receptor antagonist). Results are shown as means ± SEM. [(M) and (N)] * P < 0.05 indicates statistical significance in unpaired t tests. [(Q), (S), and (T)] ** P < 0.01 and **** P < 0.0001 indicate statistical significance in paired t tests.

Article Snippet: To test whether ERα or ERβ is necessary for the stimulatory effects of 27HC on POMC ARH neurons, brain slices were treated with 100 nM 27HC in the presence of TTX, a cocktail of synaptic inhibitors, and either BHPI (50 μM), an ERα antagonist (catalog no. 5.38005, MilliporeSigma), or PHTPP (10 μM), an ERβ antagonist (catalog no. 2662, Tocris).

Techniques: Staining, Membrane, Incubation