298198-52-4
Chemical Structure
SSR180711
- CAS No.: 298198-52-4
- Formula:C14H17BrN2O2
- Molecular Weight:325.20
InChIKey: RXLOZRCLQMJJLC-UHFFFAOYSA-N
SMILES: O=C(N1CCN2CCC1CC2)OC3=CC=C(C=C3)Br
Biological Activity: SSR180711 is an orally active, blood-brain barrier-penetrant α7-nAChR partial agonist (EC50 = 0.9-4.4 µM; Ki = 22/14 nM for binding to rat/human α7-nAChR; IC50 = 30/18 nM). SSR180711 reverses NMDA receptor antagonist-induced cognitive and latent inhibition deficits by enhancing glutamatergic and GABAergic neurotransmission, acetylcholine and Dopamine (HY-B0451) release, and long-term potentiation. SSR18071 is used in research on schizophrenia and Alzheimer's disease[1][2][3][4][5][6][7][8][9].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
SSR180711 | 99.52% | SSR180711 is an orally active, blood-brain barrier-penetrant α7-nAChR partial agonist (EC50 = 0.9-4.4 µM; Ki = 22/14 nM for binding to rat/human α7-nAChR; IC50 = 30/18 nM). SSR180711 reverses NMDA receptor antagonist-induced cognitive and latent inhibition deficits by enhancing glutamatergic and GABAergic neurotransmission, acetylcholine and Dopamine (HY-B0451) release, and long-term potentiation. SSR18071 is used in research on schizophrenia and Alzheimer's disease. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Horti AG, et al. 18F-ASEM, a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2014 Apr;55(4):672-7.
- [2]. Milienne-Petiot M, et al. Nicotine improves probabilistic reward learning in wildtype but not alpha7 nAChR null mutants, yet alpha7 nAChR agonists do not improve probabilistic learning. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 2018 Nov;28(11):1217-1231.
- [3]. Neves GA, et al. α7 Nicotinic receptor-modulating agents reverse the hyperdopaminergic tone in the MAM model of schizophrenia. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2018 Jul;43(8):1712-1720.
- [4]. Biton B, et al. SSR180711, a novel selective alpha7 nicotinic receptor partial agonist: (1) binding and functional profile. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2007 Jan;32(1):1-16. [Content Brief]
- [5]. Hashimoto K, et al. Phencyclidine-induced cognitive deficits in mice are improved by subsequent subchronic administration of the novel selective alpha7 nicotinic receptor agonist SSR180711. Biological psychiatry. 2008 Jan 01;63(1):92-7.
- [6]. Pichat P, et al. SSR180711, a novel selective alpha7 nicotinic receptor partial agonist: (II) efficacy in experimental models predictive of activity against cognitive symptoms of schizophrenia. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2007 Jan;32(1):17-34.
- [7]. Barak S, et al. Pro-cognitive and antipsychotic efficacy of the alpha7 nicotinic partial agonist SSR180711 in pharmacological and neurodevelopmental latent inhibition models of schizophrenia. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2009 Jun;34(7):1753-63.
- [8]. Hansen HH, et al. Alpha-7 nicotinic acetylcholine receptor agonists selectively activate limbic regions of the rat forebrain: an effect similar to antipsychotics. Journal of neuroscience research. 2007 Jun;85(8):1810-8.
- [9]. Kjaerby C, et al. Repeated potentiation of the metabotropic glutamate receptor 5 and the alpha 7 nicotinic acetylcholine receptor modulates behavioural and GABAergic deficits induced by early postnatal phencyclidine (PCP) treatment. Neuropharmacology. 2013 Sep;72:157-68.
