PZ0408
WAY-163909 hydrochloride
≥98% (HPLC)
别名:
(7bR,10aR)-1,2,3,4,7a,9,10,10a-Octahydro-8H-cyclopenta[4,5]pyrrolo[3,2,1-jk][1,4]benzodiazepine, hydrochloride, (7bR,10aR)-1,2,3,4,8,9,10,10a-Octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole, hydrochloride, WAY 163909 hydrochloride, WAY-162545 active isomer, WAY-909 hydrochloride, WAY163909 hydrochloride
SMILES string
Cl.N21[C@H]3[C@H](CCC3)c4c2c(ccc4)CNCC1
InChI
1S/C14H18N2.ClH/c1-3-10-9-15-7-8-16-13-6-2-4-11(13)12(5-1)14(10)16;/h1,3,5,11,13,15H,2,4,6-9H2;1H/t11-,13-;/m1./s1
InChI key
UJVFYZZBCUXMDV-LOCPCMAASA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
room temp
Quality Level
Biochem/physiol Actions
WAY-163909 is a 5-hydroxytryptamine receptor 2C (5-HT2C) agonist (EC50/Emax = 8 nM/90% vs. 185 nM/40%/5-HT2B; Ki = 10.5 nM/5-HT2C, 212 nM/5-HT2A, 343 nM/5-HT7, 485 nM/5-HT2B, 245 nM/D4, 665 nM/rat α-1, >1 μM/5-HT1A, D2, D3, rat 5-HT-T) with no 5-HT2A-stimulatory potency. WAY-163909 exhibits anorectic (ED50 in mg/kg via i.p. = 1.4/DIO mice and 5.19/Zucker rats), antipsychotic (morphine-induced mouse climbing ID50 = 10.69 mg/kg i.p.; rat avoidance responding reduction ED50 = 1.27 mg/kg i.p. and 6.50 mg/kg p.o.) and antidepressant (10 mg/kg, i.p. or s.c. in forced rat swimming test ; 3 mg/kg/day i.p. in reducing olfactory bulbectomy/BULB-induced hyperactivity in rats) efficacy in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Maylen Perez Diaz et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 44(3), 478-486 (2018-09-07)
Perseverative behavior has been highly implicated in addiction. Activation of serotonin 2C receptors (5-HT2CRs) attenuates cocaine and high caloric food intake, but whether a 5-HT2CR agonist can reduce high caloric diet (HCD) or methamphetamine (METH) intake and response perseveration remains
John Dunlop et al.
The Journal of pharmacology and experimental therapeutics, 313(2), 862-869 (2005-02-12)
The pharmacological profile of WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine (HT)(2C) (serotonin) receptor-selective agonist is presented. WAY-163909 displaced [(125)I]2,5-dimethoxy-4-iodoamphetamine binding from human 5-HT(2C) receptor sites, in Chinese hamster ovary (CHO) cell membranes, with a K(i) value of 10.5 +/- 1.1
Karen L Marquis et al.
The Journal of pharmacology and experimental therapeutics, 320(1), 486-496 (2006-10-14)
Serotonin-2C (5-HT2C) receptor antagonists and agonists have been shown to affect dopamine (DA) neurotransmission, with agonists selectively decreasing mesolimbic DA. As antipsychotic efficacy is proposed to be associated with decreased mesolimbic DA neurotransmission by virtue of DA D2 receptor antagonism
Benjamin U Phillips et al.
Psychopharmacology, 235(7), 2101-2111 (2018-04-24)
Dysregulation of the serotonin (5-HT) system is a pathophysiological component in major depressive disorder (MDD), a condition closely associated with abnormal emotional responsivity to positive and negative feedback. However, the precise mechanism through which 5-HT tone biases feedback responsivity remains
Steven M Grauer et al.
Psychopharmacology, 204(1), 37-48 (2008-12-25)
5-HT(2C) agonists, by decreasing mesolimbic dopamine without affecting nigrostriatal dopamine, are predicted to have antipsychotic efficacy with low extrapyramidal side effects (EPS). Combining 5-HT(2C) agonists with low doses of existing antipsychotics could increase treatment efficacy while reducing treatment liabilities such
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