| Identification | Back Directory | [Name]
ATC 0175 | [CAS]
510733-97-8 | [Synonyms]
ATC 0175 hydrochloride
N-[cis-4-[[4-(Dimethylamino)-2-quinazolinyl]amino]cyclohexyl]-3,4-difluorobenzamidehydrochloride | [Molecular Formula]
C23H25F2N5O.ClH | [MDL Number]
MFCD08276913 | [MOL File]
510733-97-8.mol | [Molecular Weight]
461.941 |
| Hazard Information | Back Directory | [Biological Activity]
Potent, selective and orally active melanin-concentrating hormone receptor 1 (MCH 1 ) antagonist (IC 50 values are 13.5 and > 10000 nM for MCH1 and MCH2 receptors respectively). Exhibits anxiolytic and antidepressant activity in rodents. Also displays affinity for 5-HT 2B and 5-HT 1A receptors (IC 50 values are 9.66 and 16.9 nM respectively). | [in vitro]
assays showed that this compound is a potent antagonist with a high affinity for mch1r. the receptor binding and the functional assay (mch-induced increase in [ca2+]) indicated that atc0175 is a noncompetitive antagonist at mch1rs 1. | [in vivo]
atc0175 displayed anxiolytic effects in numerous animal models of anxiety including the social interaction test, elevated plus-maze test, maternal separation-induced vocalization and stress-induced hyperthermia. in addition, atc0175 treatment also exhibited antidepressant effects in the forced swimming test 2. | [References]
1. semple g, tran ta, kramer b, et al. pyrimidine-based antagonists of h-mch-r1 derived from atc0175: in vitro profiling and in vivo evaluation. bioorganic & medicinal chemistry letters. 2009;19(21):6166-6171.2. chaki s, yamaguchi j, yamada h, et al. atc0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety. cns drug reviews. 2005;11(4):341-352. |
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BOC Sciences
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| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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