792173-99-0 Usage
Uses
SB 334867 is an orexin 1 receptor antagonist.
Biological Activity
sb-334867 free base is a selective antagonist of orexin-1 receptor [1].orexin-a and orexin-b are two peptides isolated from rat hypothalamus. they are involved in some physiological functions such as the control of feeding, energy metabolism and regulation of the sleep-wake cycle.sb-334867 free base could inhibit the orexin-a and orexin-b induced calcium responses in cho-ox1 cells with pkb values of 7.27 and 7.23, respectively. sb-334867 was more selective for ox1 receptor over ox2 receptor. it caused 32.7% and 22% inhibition of orexin-a and orexin-b induced calcium responses in cho-ox2 cells, respectively. moreover, sb-334867 was found to reduce both orexin-a-induced and fasting-induced food intake. the acute anorectic effect of it was associated with significant reductions in all active behaviours [1, 2].
Biochem/physiol Actions
Lateral hypothalamic orexin neuron activation leads to the development of morphine conditioned place preference, which is preferably blocked by SB-334867.
references
[1] smart d, sabido-david c, brough s j, et al. sb-334867-a: the first selective orexin-1 receptor antagonist. british journal of pharmacology, 2001, 132(6): 1179-1182.[2] rodgers r j, halford j c g, nunes de souza r l, et al. sb-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-a in rats. european journal of neuroscience, 2001, 13(7): 1444-1452.
Check Digit Verification of cas no
The CAS Registry Mumber 792173-99-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,9,2,1,7 and 3 respectively; the second part has 2 digits, 9 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 792173-99:
(8*7)+(7*9)+(6*2)+(5*1)+(4*7)+(3*3)+(2*9)+(1*9)=200
200 % 10 = 0
So 792173-99-0 is a valid CAS Registry Number.
InChI:InChI=1/C17H13N5O2/c1-10-20-12-5-4-11(9-15(12)24-10)21-17(23)22-14-6-8-18-13-3-2-7-19-16(13)14/h2-9H,1H3,(H2,18,21,22,23)
792173-99-0Relevant articles and documents
Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: Possible confounding effects on in vivo and in vitro studies
McElhinny Jr., Charles J.,Lewin, Anita H.,Mascarella, S. Wayne,Runyon, Scott,Brieaddy, Lawrence,Carroll, F. Ivy
, p. 6661 - 6664 (2013/01/14)
SB-334867 has been an important ligand for the study of the orexin 1 (OX1) receptor due to its high OX1/OX2 selectivity and bioavailability. This ligand however, contains a 2-methylbenzoxazole ring system which is known to undergo hydrolysis, particularly under acidic or basic conditions. The possibility that SB-334867 would be susceptible to significant hydrolysis was evaluated in various formulations and in the solid state. SB-334867 was found to be unstable under conditions commonly employed to prepare stock solutions for in vitro and in vivo studies. In addition, and most alarmingly, the hydrochloride salt of SB-334867 was found to quantitatively decompose to an OX1-inactive product even in the solid state. These findings combine to suggest that studies using SB-334867 (and any other 2-methylbenzoxazole-containing compound) should be performed with great care to avoid the confounding effects of the rapid hydrolytic decomposition of this susceptible structure.
