Use of norepinephrine reuptake modulators for preventing and treating vasomotor symptoms
A technology of norepinephrine, epinephrine, used in the field of prevention and treatment of vasomotor disease
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Embodiment 1
[0135] In preclinical models of vasomotor instability, NRIs are effective in attenuating vasomotor instability Fixed effect
[0136] The method described in the morphine-dependent rat model in the General Methods section was used except that the rats were injected subcutaneously with vehicle (sterile water) or desipramine 1 hour before administration of naloxone. ), the desipramine can be prepared as described in US Patent Publication No. 2002 / 0107249, dissolved in sterile water and administered at 0.1, 1.0, 10 and 30 mg / kg ( image 3 A). Desipramine dose-dependently attenuated naloxone-induced hot flashes at the site of maximal hot flashes (15 minutes after naloxone administration; Δ°C, mean + SEM).
[0137] Subcutaneous injection of vehicle (sterile water) or desipramine (dissolved in sterile water and administered at 10 mg / kg) to rats ( image 3 B). In a telemetry model of OVX-induced thermoregulatory disturbances, changes in TST over time (Δ°C, mean + SEM) demonstra...
Embodiment 2
[0142] Alleviating effect of NRI combined with SRI on vasomotor instability
[0143]The method described in the morphine-dependent rat model in the General Methods section was used except that the rats were injected subcutaneously with vehicle (sterile water), desipramine 1 hour before administration of naloxone ) (prepared as described in US-A-3,454,554, dissolved in sterile water and administered at 0.1, 1.0, 10 mg / kg) or fluoxetine (fluoxetine) (Sigma, dissolved in sterile water, administered at 10, 30 , 60 mg / kg administration), or a combination of fluoxetine at 10 mg / kg and desipramine in increasing doses as listed above.
[0144] At the point of maximum hot flashes (15 minutes after naloxone administration; Δ°C, mean + SEM), desipramine dose-dependently attenuated naloxone-induced hot flashes in the MD model, but caused A slight slope of the evaluation line (solid line, Figure 4 ). The slight slope of the evaluation line is characteristic of compounds with multisit...
Embodiment 3
[0146] Alleviation of vasomotor instability by compounds with dual NRI / SRI activity
[0147] The method described in the morphine-dependent rat model in the General Methods section was adopted, except that the rats were subcutaneously injected with vehicle (sterile water), venlafaxine ( venlafaxine) (dissolved in sterile water and administered at 1.0, 10, 20, 40 mg / kg) or DVS-233 (dissolved in sterile water and administered at 1.0, 10, 30, 60 mg / kg). Venlafaxine and DVS-233 were synthesized as described in US-A-4,535,186. At the point of maximum hot flash (15 minutes after administration of naloxone; Δ°C, mean + SEM), venlafaxine dose-dependently (ED 50 Value = 15+7mg / kg) alleviated naloxone (naloxone)-induced hot flashes ( Figure 5 A). DVS-233 dose-dependently (ED 50 Value = 30+3mg / kg) alleviated naloxone (naloxone)-induced hot flashes ( Figure 5 B).
[0148] Figure 5 Methods for C and 5D were as described within the telemetry model in the general methods section....
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