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- W2046272484 abstract "Alzheimer's disease (AD) is a neurodegenerative disorder of aged population leading to cognitive decline and ultimately death. The current population with dementia is about 36 million of which half the population has Alzheimer's disease. Drawback of the current therapies includes cholinergic side effect and lack of efficacy in advance stages of the disease. M 1 -PAM may hold promise in the alleviation of AD with few side effect and better efficacy. The selectivity panel reveals an affinity for M 1 receptor in comparison to M 2 -M 5 receptor. SUVN-I1307014 was assessed by reporter gene assay against various muscarinic receptor sub-types M 2, M 3 and M 5. SUVN-I1307014 was assessed for agonist activity up to the maximal tested concentration of 10μM. SUVN-I1307014 was also assessed in radio ligand binding study upto 10μM. Pharmacokinetic profile and brain penetration was studied in male Wistar rats. Efficacy of SUVN-I1307014 was assessed in various cognitive tasks such as object recognition task (ORT) and fear conditioning assay In the functional reporter gene assay at human M 1 muscarinic receptor, SUVN-I1307014 shifted acetylcholine dose response towards leftward with a 17 fold shift of acetylcholine potency at 10μM and an EC 50 (inflection point) of 560 nM, which proves that SUVN-I1307014 is a potent positive allosteric modulator of human M 1 muscarinic receptor. SUVN-I1307014 did not show any binding affinity up to the maximal tested concentration of 10μM, towards muscarinic receptor subtypes M 1, M 2, M 3 and M 4. SUVN-I1307014 reversed episodic memory deficits in object recognition task and memory deficits induced by scopolamine in fear conditioning assay.It had favorable pharmacokinetic profile and adequate brain penetration in male Wistar rats. SUVN-I1307014 is a novel, potent, selective, orally bioavailable and efficacious M 1 -PAM that holds promise in the treatment of AD and dementia. SUVN-I1307014 is being further evaluated for various safety parameters." @default.
- W2046272484 created "2016-06-24" @default.
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- W2046272484 date "2014-07-01" @default.
- W2046272484 modified "2023-09-27" @default.
- W2046272484 title "P1-399: SUVN-I1307014: NOVEL M1 MUSCARINIC ACETYLCHOLINE RECEPTOR POSITIVE ALLOSTERIC MODULATOR FOR POTENTIAL TREATMENT OF ALZHEIMER'S DISEASE" @default.
- W2046272484 doi "https://doi.org/10.1016/j.jalz.2014.05.641" @default.
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