The neurokinin NK2 antagonist, saredutant, ameliorates stress-induced conditions without impairing cognition

Rogacki, Nancy; Lopez-Grancha, Mati; Naimoli, Vanessa; Potestio, Lisa; Stevens, Rachel J.; Pichat, Philippe; Bergis, Olivier; Cohen, Caroline; Varty, Geoffrey B.

doi:10.1016/j.pbb.2010.11.017

Cited by 9 publications

(3 citation statements)

References 29 publications

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“…In the following study; the board hole tests (BHT) showed that: the induced diabetes reduced the cognition of the rats in parameters of Latency of the First Head Dipping (LFHD) in seconds, number of head dipping (NHD) and duration of head dipping (DHD) from (100%) 35 s to (60%) 22.4 s, from (100%) 9.6 times to (58.3%) 5.6 times, and from (100%) 20 s to (50%) 10 s respectively; while its improved in AHA and insulin treated rats to (92.6%) 32.4 s, (108.3%) 10.4 times, (123%) 24.6 s, and ((114.3%) 40 s., (133.3%) 12.8 times, and (128%) 25.6 s)) respectively as shown in Figure 1, same results have been highlighted by Rogacki et al, [36] in which they stated that: the healthy animals take longer time to begin the first head dipping. The exploratory activity was reduced in diabetic non treated rats from (100%) 1440 cm to (63.9%) 920 cm while AHA and Insulin treated rats increased to (88.9%) 1280 cm, and (108.3%) 1560 cm respectively as shown in Figure 2, in the same realm Deacon et al, [37] found the decrement of exploratory activity which indicates the impairment in motor Figure 3, such result has been mentioned in the introduction section by Moriera et al, [38] and Brown et al, [35].…”

Section: Discussionsupporting

confidence: 83%

Evaluation of Diabetic Rats Behavior after Treatment by <i>Artemisia herba-alba</i> Relative to Insulin

Bushara¹,

Ali²,

Omer³

et al. 2017

JDM

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The aim of the study was to evaluate the behavioral signs of diabetic rats after treatment by Artemisia herba-alba (AHA) and insulin. Method: Based on the induction of diabetes in wistar rats by intraperitoneal (I/P) injection of 60 mg/kg streptozotocin (STZ), then treated by AHA as 20 mg (I/P) and insulin subcutaneously (S/C). The samples of rats were: 1) Diabetic control, 2) Injected with insulin, 3) Injected with AHA, 4) Non diabetic rats, which were fostered for 21 day; then weighted and the behavioral tests were conducted. Results: The board hole tests (BHT) showed that: the induced diabetes reduced the cognition of the rats in view of Latency of the First Head Dipping (LFHD) in seconds, number of head dipping (NHD) and duration of head dipping (DHD) by 49.3%, while it's improved in AHA and insulin treated rats by 52% and 69% in average respectively. The exploratory activity reduced in diabetic rats by 36%, while AHA and Insulin treated rats increased by 53% and 72% respectively. The rearing test showed an increase of anxiety among diabetic in form of duration of rearing, number of rearing and time spend in center by 51.7% in average respectively, while the anxiety reduced after treatment by AHA and insulin by 39% and 47.3% in average respectively. Also the diabetes increased the depression state by 106%, while the treatment by AHA and insulin reduced the depression state by 77% and 88% respectively. And VPT showed that: motor impairment occurred in diabetic cases and improved after AHA and insulin treatment.

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Section: Discussionsupporting

confidence: 83%

Evaluation of Diabetic Rats Behavior after Treatment by <i>Artemisia herba-alba</i> Relative to Insulin

Bushara¹,

Ali²,

Omer³

et al. 2017

JDM

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“…Saredutant (SR48968) is a selective, non-peptide, neurokinin-2 (NK 2 ) receptor antagonist that exhibits antidepressant/anxiolytic activity in rodents, lacking side-effects such as sedation, disinhibition or memory impairment Louis et al 2008 ;Micale et al 2008b ;Overstreet et al 2010 ;Rogacki et al 2011 ;Salomé et al 2006). Little is known of the mechanism(s) underlying saredutant antidepressant/ anxiolytic activity.…”

Section: Introductionmentioning

confidence: 99%

Behavioural and neurochemical changes induced by stress-related conditions are counteracted by the neurokinin-2 receptor antagonist saredutant

Tamburella

Leggio

Micale

et al. 2013

International Journal of Neuropsychopharmacology

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These experiments were undertaken to assess the mechanisms underlying the antidepressant-like effects of the neurokinin-2 (NK(2)) receptor antagonist saredutant (SR48968) in rats tested in the forced swim test (FST), by analysing hippocampal brain-derived neurotrophic factor (BDNF) and plasma corticosterone [as index of hypothalamic-pituitary-adrenal (HPA) axis activity]. Male Wistar rats received three intraperitoneal injections over 24 h of vehicle, saredutant (5 mg/kg), citalopram (15 mg/kg), clomipramine (50 mg/kg). Rats were subjected to restraint stress (4 h) 24 h prior to the FST procedure. This stress procedure increased immobility and decreased swimming behaviour in the FST; furthermore, it lowered hippocampal BDNF protein expression and increased plasma corticosterone levels. Saredutant and clomipramine or citalopram, used here as positive controls, reduced the immobility time in the FST both under basal conditions and after stress exposure. This effect was not attributable to changes in locomotion, because locomotor activity was unchanged when assessed in the open field test. Pretreatment with para-cholorophenylalanine (150 mg/kg, 72 h and 48 h prior to FST) abolished the effect of citalopram and saredutant on immobility time. At neurochemical level, saredutant attenuated activation of HPA axis in stressed animals more than clomipramine or citalopram. The behavioural effects of saredutant support the hypothesis that NK(2) receptor activity is involved in stress-related disorders. These effects of saredutant may be related to normalization of the HPA axis. Moreover, saredutant increases BDNF expression in the hippocampus, confirming the role of NK(2) receptor blockade in BDNF activation following stressor application.

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“…The rapid synthesis of proposed metabolites of drug candidates often requires innovative solutions to synthetically challenging problems. Indeed, during the development of saredutant , hydroxypiperidinone 1 (Scheme ) was isolated from metabolism studies, and an authentic sample was needed for confirmation of the structural assignment. Many de novo approaches were considered and attempted without success.…”

Section: Introductionmentioning

confidence: 99%

An Oxidative Approach to a Hydroxypiperidinone Utilizing a Rh-Catalyzed C-H Activation Process

Ayers

2013

J. Heterocyclic Chem.

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The neurokinin NK2 antagonist, saredutant, ameliorates stress-induced conditions without impairing cognition

Cited by 9 publications

References 29 publications

Evaluation of Diabetic Rats Behavior after Treatment by <i>Artemisia herba-alba</i> Relative to Insulin

Evaluation of Diabetic Rats Behavior after Treatment by <i>Artemisia herba-alba</i> Relative to Insulin

Behavioural and neurochemical changes induced by stress-related conditions are counteracted by the neurokinin-2 receptor antagonist saredutant

An Oxidative Approach to a Hydroxypiperidinone Utilizing a Rh-Catalyzed C-H Activation Process

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The neurokinin NK2 antagonist, saredutant, ameliorates stress-induced conditions without impairing cognition

Cited by 9 publications

References 29 publications

Evaluation of Diabetic Rats Behavior after Treatment by &lt;i&gt;Artemisia herba-alba&lt;/i&gt; Relative to Insulin

Evaluation of Diabetic Rats Behavior after Treatment by &lt;i&gt;Artemisia herba-alba&lt;/i&gt; Relative to Insulin

Behavioural and neurochemical changes induced by stress-related conditions are counteracted by the neurokinin-2 receptor antagonist saredutant

An Oxidative Approach to a Hydroxypiperidinone Utilizing a Rh-Catalyzed C-H Activation Process

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Evaluation of Diabetic Rats Behavior after Treatment by <i>Artemisia herba-alba</i> Relative to Insulin

Evaluation of Diabetic Rats Behavior after Treatment by <i>Artemisia herba-alba</i> Relative to Insulin