162760-96-5 Usage
Biological Activity
5-ht1a receptors mediate various serotonergic functions and may be implicated in various pathologies including depressive and anxiety disorders, alzheimer’s disease, and schizophrenia. way-100635 is a potential spect ligands for the 5-ht1a receptor.
in vitro
way-100635 displaced specific binding of the 5-ht1a radioligand, [3h]8-oh-dpat, to rat hippocampal membranes with a plc50 of 8.87. in functional assays, way-100635 was a potent 5-ht1a receptor antagonist, with no evidence of any 5-htia receptor agonist or partial agonist activity. in the isolated guinea-pig ileum way-100635 was a potent and, at high concentrations, an insurmountable antagonist of the 5-ht1a receptor agonist action of 5-carboxamidotryptamine, with an apparent pa 2 value (at 0.3 nm) of 9.71 [2].
in vivo
way-100635 blocked the inhibitory action of 8-oh-dpat on dorsal raphe neuronal firing in the anaesthetised rat at doses which had no inhibitory action per se. in behavioural models, way-100635 itself induced no overt behavioural changes but potently antagonised the behavioural syndrome induced by 8-oh-dpat in the rat and guinea-pig (minimum effective dose = 0.003 mg/kg s.c. and id50 = 0.01 mg/kg s.c., respectively). way-100635 also blocked the hypothermia induced by 8-oh-dpat in the mouse and rat with id50 values of 0.01 mg/kg s.c. [2].
references
[1] al hussainy r, verbeek j, van der born d, braker ah, leysen je, knol rj, booij j, herscheid jk. design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of n-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-n-(pyridin-2-yl)cyclohexanecarboxamide (way-100635) as potential spect ligands for the 5-ht1a receptor. j med chem. 2011;54(10):3480-91. [2] forster ea, cliffe ia, bill dj, dover gm, jones d, reilly y, fletcher a. a pharmacological profile of the selective silent 5-ht1a receptor antagonist, way-100635. eur j pharmacol. 1995;281(1):81-8.
Check Digit Verification of cas no
The CAS Registry Mumber 162760-96-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,6,2,7,6 and 0 respectively; the second part has 2 digits, 9 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 162760-96:
(8*1)+(7*6)+(6*2)+(5*7)+(4*6)+(3*0)+(2*9)+(1*6)=145
145 % 10 = 5
So 162760-96-5 is a valid CAS Registry Number.
162760-96-5Relevant articles and documents
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors
Mangin, Floriane,Dilly, Sebastien,Joly, Benoit,Scuvee-Moreau, Jacqueline,Evans, Jon,Setola, Vincent,Roth, Bryan L.,Liegeois, Jean-Francois
supporting information; experimental part, p. 4550 - 4554 (2012/08/08)
The selectivity for 5-HT1A versus D4 receptors is significantly increased when the basic side chain of WAY-100635 is replaced by a 4-phenylpiperazine (3e) or a 4-phenyl-1,2,3,6-tetrahydropyridine moiety (3i). The 4-phenyl-1,2,3,6-tet
USE OF 5-HT 1A? RECEPTOR ANTAGONISTS FOR THE TREATMENT OF URINARY INCONTINENCE
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, (2008/06/13)
Compounds which: (a) bind to a 5-HT1A receptor with an affinity of at least 10M, (b) bind to a 5-HT1A receptor with an affinity at least 50-fold stronger than the affinity with which the compound binds to an alpha 1-adrenergic receptor, and (c) exhibi
USE OF 5-HT1A RECEPTOR ANTAGONISTS FOR THE TREATMENT OF URINARY INCONTINENCE
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, (2008/06/13)
The present invention discloses compositions and methods for treating neuromuscular dysfunction of the lower urinary tract in mammals, including humans, using serotonin 5-HT 1A receptor antagonist compounds that exert their inhibitory effects via pre-syna
