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Tomokazu Nakako
Dainippon Sumitomo Pharma Co., Ltd.
16Publications
7H-index
118Citations
Publications 16
Newest
#1Manato KotaniH-Index: 4
#2Kohei ShimonoH-Index: 1
Last.Kazuhito IkedaH-Index: 6
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Abstract Eye tracking systems are used to investigate eyes position and gaze patterns presumed as eye contact in humans. Eye contact is a useful biomarker of social communication and known to be deficient in patients with autism spectrum disorders (ASDs). Interestingly, the same eye tracking systems have been used to directly compare face scanning patterns in some non-human primates to those in human. Thus, eye tracking is expected to be a useful translational technique for investigating not onl...
Abstract Antagonism of the dopamine D 3 receptor is considered a promising strategy for the treatment of cognitive impairment associated with schizophrenia. We have previously reported that the atypical antipsychotic blonanserin, a dopamine D 2 /D 3 and serotonin 5-HT 2A receptor antagonist, highly occupies dopamine D 3 receptors at its antipsychotic dose range in rats. In the present study, we evaluated the effects of blonanserin on executive function in common marmosets using the object retrie...
Eye blinking is a spontaneous behavior observed in all mammals, and has been used as a well-established clinical indicator for dopamine production in neuropsychiatric disorders, including Parkinson’s disease and Tourette syndrome [1] ; [2]. Pharmacological studies in humans and non-human primates have shown that dopamine agonists/antagonists increase/decrease eye blinking rate. Common marmosets (Callithrix jacchus) have recently attracted a great deal of attention as suitable experimental animal...
Abstract We designed and synthesized a series of dihydroquinazolinone derivatives as selective M 1 and M 4 muscarinic acetylcholine receptors agonists. Introduction of the N -carbethoxy piperidine unit into a HTS hit compound followed by optimization of the amine linker and the carbamoyl moiety led to the identification of compound 1 as a potential candidate. The identified compound 1 showed high selectivity for M 1 and M 4 muscarinic acetylcholine receptors with M 4 partial agonistic activity. ...
Abstract Previous pilot clinical studies have shown that the serotonin 5-HT 1A receptor agonist tandospirone has beneficial effect on cognitive deficits associated with schizophrenia. In the present study, we evaluated the cognitive efficacy of tandospirone, given alone or in combination with the antipsychotic blonanserin, risperidone or haloperidol, on executive function in marmosets using the object retrieval with detour (ORD) task. Treatment with tandospirone alone at 20 and 40 mg/kg increase...
Abstract Infants with autism have difficulties performing joint visual attention (JVA), defined as following another person's pointing gesture and gaze. Some non-human primates (NHPs) can also perform JVA. Most preclinical research on autism spectrum disorders (ASD) has used rodents as animal models of this social interaction disorder. However, models using rodents fail to capture the complexity of social interactions that are disrupted in ASD. Therefore, JVA impairment in NHPs might be a more u...
#1Kentaro Takai (Dainippon Sumitomo Pharma Co., Ltd.)H-Index: 5
#2Yasunao Inoue (Dainippon Sumitomo Pharma Co., Ltd.)H-Index: 3
Last.Takaaki Sumiyoshi (Dainippon Sumitomo Pharma Co., Ltd.)H-Index: 6
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We designed and synthesized novel N -substituted 7-azaindoline derivatives as selective M 1 and M 4 muscarinic acetylcholine receptors (mAChRs) agonists. Hybridization of compound 2 with the HTS hit compound 5 followed by optimization of the N -substituents of 7-azaindoline led to identification of compound 1 , which showed highly selective M 1 and M 4 mAChRs agonistic activity, weak human ether-a-go-go related gene inhibition, and good bioavailability in multiple animal species.
#1Atsushi Suwa (Dainippon Sumitomo Pharma Co., Ltd.)H-Index: 4
#2Yasuko Konishi (Dainippon Sumitomo Pharma Co., Ltd.)H-Index: 4
Last.Takaaki Sumiyoshi (Dainippon Sumitomo Pharma Co., Ltd.)H-Index: 6
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We designed and synthesized novel N -sulfonyl-7-azaindoline derivatives as selective M 4 muscarinic acetylcholine receptor agonists. Modification of the N -carbethoxy piperidine moiety of compound 2 , an M 4 muscarinic acetylcholine receptor (mAChR)-preferring agonist, led to compound 1 , a selective M 4 mAChR agonist. Compound 1 showed a highly selective M 4 mAChR agonistic activity with weak hERG inhibition in vitro. A pharmacokinetic study of compound 1 in vivo revealed good bioavailability a...
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