5-HT2A receptor modulators(Serotonin 2a (5-HT2a) receptor modulators), 5-HT7 receptor modulators(Serotonin 7 (5-HT7) receptor modulators), D2 receptor modulators(Dopamine D2 receptor modulators)

+ [1]

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Behavioural disordersPsychotic Disorders

Originator Organization

Egis Gyógyszergyár Zrt.

Active Organization-

Inactive Organization

Les Laboratoires Servier SAS

Drug Highest PhasePendingPhase 1

First Approval Date-

Regulation-

Structure

Molecular FormulaC19H21ClFN5O2

InChIKeyBQNLTXZVZWVEDX-UHFFFAOYSA-N

CAS Registry494861-87-9

100 Clinical Results associated with EGIS-11150

100 Translational Medicine associated with EGIS-11150

100 Patents (Medical) associated with EGIS-11150

Literatures (Medical) associated with EGIS-11150

01 Jan 2013·NeuropharmacologyQ2 · MEDICINE

Egis-11150: A candidate antipsychotic compound with procognitive efficacy in rodents

Q2 · MEDICINE

Article

Author: István Gacsályi ; Péter Varga ; Krisztina Móricz ; József Haller ; Michael Spedding ; Gábor Gigler ; György Lévay ; Judit Bíró ; Katalin Nagy ; József Barkóczy ; Szabolcs Kertész ; Katalin Pallagi ; Ferenc A. Antoni ; Gábor Szénási ; László G. Hársing

Classical antipsychotics, e.g. haloperidol, chlorpromazine, are potent at controlling the positive symptoms of schizophrenia but frequently elicit extrapyramidal motor side-effects. The introduction of atypical antipsychotics such as risperidone, olanzapine and clozapine has obviated this problem, but none of the current drugs seem to improve the cognitive deficits accompanying schizophrenia. Thus there is an unmet need for agents that not only suppress the psychotic symptoms but also ameliorate the impairment of cognition. Here, we report the preclinical properties of a candidate antipsychotic, Egis-11150, that shows marked pro-cognitive efficacy. Egis-11150 displayed high affinity for adrenergic α(1), α(2c), 5-HT(2A) 5-HT₇, moderate affinity for adrenergic α(2a) and D₂ receptors. It was a functional antagonist on all of the above receptors, with the exception of 5-HT₇ receptors, where it was an inverse agonist. Phencyclidine-induced hypermotility in mice and inhibition of conditioned avoidance response in rats were assessed to estimate efficacy against the positive and social withdrawal test in rats was used to predict efficacy against the negative symptoms of schizophrenia. Passive-avoidance learning, novel object recognition and radial maze tests in rats were used to assess pro-cognitive activity, while phencyclidine-induced disruption of prepulse inhibition in mice was examined to test for effects on attention. Egis-11150 (0.01-0.3 mg/kg, ip.) was effective in all of the preclinical models of schizophrenia examined. Moreover, a robust pro-cognitive profile was apparent. In summary, work in preclinical models indicates that Egis-11150 is a potential treatment for controlling the psychosis as well as the cognitive dysfunction in schizophrenia. This article is part of a Special Issue entitled 'Cognitive Enhancers'.

CellsQ3 · BIOLOGY

Phenotypical Screening on Neuronal Plasticity in Hippocampal-Prefrontal Cortex Connectivity Reveals an Antipsychotic with a Novel Profile

Q3 · BIOLOGY

ArticleOA

Author: Whittington, Miles A ; Lambert, Jeremy J ; Sebban, Claude ; Spedding, Michael ; Schenker, Esther ; Jay, Thérèse M ; Etherington, Lori-An ; Szénási, Gabor ; Megyeri, Katalin ; Lévay, György I ; Chazot, Paul ; Cunningham, Mark O ; Gacsályi, Istvan ; Barkóczy, Jozsef ; Hársing, Laszlo G ; Antoni, Ferenc A ; Rocher, Cyril ; Tesolin-Decros, Brigitte ; Thomson, Ian

Dysfunction in the hippocampus-prefrontal cortex (H-PFC) circuit is a critical determinant of schizophrenia. Screening of pyridazinone-risperidone hybrids on this circuit revealed EGIS 11150 (S 36549). EGIS 11150 induced theta rhythm in hippocampal slice preparations in the stratum lacunosum molecular area of CA1, which was resistant to atropine and prazosin. EGIS 11150 enhanced H-PFC coherence, and increased the 8–9 Hz theta band of the EEG power spectrum (from 0.002 mg/kg i.p, at >30× lower doses than clozapine, and >100× for olanzapine, risperidone, or haloperidol). EGIS 11150 fully blocked the effects of phencyclidine (PCP) or ketamine on EEG. Inhibition of long-term potentiation (LTP) in H-PFC was blocked by platform stress, but was fully restored by EGIS 11150 (0.01 mg/kg i.p.), whereas clozapine (0.3 mg/kg ip) only partially restored LTP. EGIS 11150 has a unique electrophysiological profile, so phenotypical screening on H-PFC connectivity can reveal novel antipsychotics.

100 Deals associated with EGIS-11150

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Indication	Highest Phase	Country/Location	Organization	Date
Behavioural disorders	Phase 1	-	Les Laboratoires Servier SAS	-
Psychotic Disorders	Phase 1	-	-	-

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