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AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist ( K i of 153 pM), with slightly lesser potency toward 5-HT6 , 5-HT2A , and 5HT-2C receptors ( K i values of 2.04 nM, 1.56 ?nM, and 1.17? nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 ( K i of 0.58 nM) and adrenergic α2A , α2B , and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1061354-48-0. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-117046A.
AVN-101 hydrochloride
AVN-101 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT7, 5-HT2C, 5-HT2A, and 5-HT6 (Kis = 0.153, 1.17, 1.56, and 2.04 nM, respectively). It is also an antagonist of α2A-, α2B-, α2C-, α1B-, α1A-, and α1D-adrenergic receptors (Kis = 0.41, 1.77, 3.55, 9.4, 18.9, and 30.2 nM, respectively), as well as histamine H1 and H2 (Kis = 0.58 and 89 nM, respectively), but not H3, receptors. It is a multi-target drug candidate for the treatment of CNS disorders. Synonyms: 2,8-Dimethyl-5-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole hydrochloride; AVN-101 HCl; 1H-Pyrido(4,3-b)indole, 2,3,4,5-tetrahydro-2,8-dimethyl-5-(2-phenylethyl)-, hydrochloride (1:1); 2,8-dimethyl-5-(2-phenylethyl)-1H,2H,3H,4H,5H-pyrido[4,3-b]indole hydrochloride; 2,3,4,5-tetrahydro-2,8-dimethyl-5-(2-phenylethyl)-1H-pyrido[4,3-b]indole, monohydrochloride. Grades: ≥95%. CAS No. 1061354-48-0. Molecular formula: C21H25ClN2. Mole weight: 340.90.
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