Dilept - CAS 200954-39-8
Category: Inhibitor
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Dopamine Receptor | Neurotensin Receptor
Dilept is an antagonist of neurotensin (NT) and dopamine (DA) receptor used to mitigate positive and negative symptoms of schizophrenia.
Brife Description:
Neurotensin and dopamine receptor antagonist
N-caproyl-l-prolyl-l-tyrosine methyl ester; methyl (2S)-2-[[(2S)-1-hexanoylpyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoate
schizophrenia treatment
Canonical SMILES:
1.[The study of procognitive effect of the potential antipsychotic, Dilept and its main metabolite, GZR-125 at the novel objects recognition test in rats].
Gorelov PI;Ostrovskaia RU;Sazonova NM Eksp Klin Farmakol. 2013;76(7):3-5.
The effect of dipeptidal neurotensine mimetic, N-caproyl-L-prolyl-L-tyrosine methyl ester (GZR-123, Dilept) and its main metabolite N-caproyl-L-prolyl-L-tyrosine (GZR-125) was evaluated at novel objects recognition test (NOR) in the male outbred rats. NOR was chosen from many cognitive test as those involving the selective action on the attention and episodic memory and considering as translational model for the study of cognition deficiency in schizophrenics. M-cholinoblocking agent scopolamine (0.2 mg/kg s.c.) was used as agent disturbing the performance of the test. Dilept (2 mg/kp i.p.) was shown to restore the NOR performance, disturbed by scopolamine. The same was true for GZR-125 (2 mg/kp i.p.), whose cholinopositive effect could contribute to the procognitive effect of the parent molecule.
2.Neuromodulatory mechanism underlying the effect of the atypical dipeptide neuroleptic dilept.
Retyunskaya MV;Guzevatykh LS;Bondarenko NA;Gudasheva TA;Ostrovskaya RU;Voronina TA Bull Exp Biol Med. 2003 Nov;136(5):467-70.
We studied the effects of a new dipeptide neuroleptic Dilept (N-caproyl-L-prolyl-L-tyrosine methyl ester) on activity of neurotransmitter systems in the brain. Dilept possessed antidopamine, glutamate modulatory, and cholinomimetic properties. These data indicate that Dilept is of potential efficacy in relieving positive and negative symptoms of schizophrenia.
3.Comparison of antipsychotic activity and discriminative stimulus effects of the novel acylprolyltyrosine containing compound, GZR-123, and sulpiride.
Asmakova LS;Kalinina TS;Ostrovskaya RU;Gudasheva TA;Zaitseva NI;Bondarenko NA;Voronina TA;Seredenin SB Pharmacol Biochem Behav. 1999 Oct;64(2):359-62.
The present experiment has been performed to determine the pharmacological profile of a newly synthesized systematically active prolyltyrosine containing compound, caproyl-L-Pro-L-Tyr methyl ester (GZR-123), and to compare it with that of the standard atypical benzamide neuroleptic, sulpiride. GZR-123 demonstrated antagonistic activity on apomorphine-induced climbing and on L-DOPA-dependent extrapolatory behavior in dose ranging between 0.4-4.0 mg/kg i.p.. It did not provoke a cataleptogenic effect or lethality, even at doses much higher than those causing antidopamine effects (more than 500 mg/kg). The effective doses of sulpiride in the above-listed antidopamine tests were shown to be 17.5 and 16.0 mg/kg i.p. correspondingly. Although these doses of sulpiride did not demonstrate cataleptogenic effects, an increase of the dose level to 120 mg/kg induced pronounced catalepsy. Both GZR-123 (6 mg/kg) and sulpiride (40 and 60 mg/kg) were investigated by training rats to discriminate each of them from saline in a two-lever, water-reinforcement operant procedure. Both GZR-123 and sulpiride demonstrated weak discriminability in this task. GZR-123 increased drug-associated lever selection when administered in doses of 2 and 6 mg/kg, for sulpirirde these doses were demonstrated to be 25-60 mg/kg.
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