CAS 792173-99-0|SB 334867

Introduction：Basic information about CAS 792173-99-0|SB 334867, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. SB 334867 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	SB 334867
CAS Number	792173-99-0	Molecular Weight	319.317
Density	1.4±0.1 g/cm3	Boiling Point	549.5±58.0 °C at 760 mmHg
Molecular Formula	C₁₇H₁₃N₅O₂	Melting Point	/
MSDS	ChineseUSA	Flash Point	286.1±32.3 °C
Symbol	GHS07	Signal Word	Warning

Names

Name	1-(2-Methyl-1,3-benzoxazol-6-yl)-1-(1,5-naphthyridin-4-yl)urea
Synonym	More Synonyms

SB 334867 BiologicalActivity

Description	SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.IC50 value: 7.2 (pKb) [1]Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on the UTP (3 microM)-induced calcium response in CHO-OX(1) cells. SB-334867-A (10 microM) also inhibited OX(2) mediated calcium responses (32.7+/-1.9% versus orexin-A) [1].in vivo: Single-unit recordings in anesthetized rats demonstrated the central effects of the selective orexin-1 receptor antagonist SB-334867 (2 mg/kg, intravenous), as it reversed the excitatory effects of orexin-A administration (6 microg, intracerebroventricular) on the activity of locus coeruleus (LC) cells [2]. The ICV injection of SB-334867 alone had no effect on the formalin-induced nociceptive behaviors. Pre-treatment with SB-334867 at a dose of 0.5 nmol significantly attenuated the analgesia induced by morphine (at dose 1.5mg/kg of morphine; interphase and phase 2B and at dose 3mg/kg of morphine just phase 2B of formalin test) [3]. Administered alone, SB-334867 (30 mg/kg, but not lower doses) significantly reduced food intake and most active behaviours (eating, grooming, sniffing, locomotion and rearing), while increasing resting. Pretreatment with SB-334867 dose-dependently blocked these effects of orexin-A, with significant antagonism evident at dose levels (3-10 mg/kg) below those required to produce intrinsic behavioural effects under present test conditions in rats [4].Toxicity: Acute systemic treatment with the selective orexin-1 (OX1R) antagonist SB-334867 reduces food intake in rats, an effect associated with an acceleration in behavioural satiety and unrelated to gross behavioural disruption, alterations in palatability, or toxicity.
Related Catalog	Signaling Pathways >>GPCR/G Protein >>Orexin Receptor (OX Receptor)Research Areas >>Neurological Disease
References	[1]. Smart D, et al. SB-334867-A: the first selective orexin-1 receptor antagonist. Br J Pharmacol. 2001 Mar;132(6):1179-82. [2]. Rasmussen K, et al. The orexin-1 receptor antagonist SB-334867 blocks the effects of antipsychotics on the activity of A9 and A10 dopamine neurons: implications for antipsychotic therapy. Neuropsychopharmacology. 2007 Apr;32(4):786-92. [3]. Azhdari-Zarmehri H, et al. Orexin receptor type-1 antagonist SB-334867 decreases morphine-induced antinociceptive effect in formalin test. Pharmacol Biochem Behav. 2013 Nov;112:64-70. [4]. Rodgers RJ, et al. SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats. Eur J Neurosci. 2001 Apr;13(7):1444-52.

Description

SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.IC50 value: 7.2 (pKb) [1]Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on the UTP (3 microM)-induced calcium response in CHO-OX(1) cells. SB-334867-A (10 microM) also inhibited OX(2) mediated calcium responses (32.7+/-1.9% versus orexin-A) [1].in vivo: Single-unit recordings in anesthetized rats demonstrated the central effects of the selective orexin-1 receptor antagonist SB-334867 (2 mg/kg, intravenous), as it reversed the excitatory effects of orexin-A administration (6 microg, intracerebroventricular) on the activity of locus coeruleus (LC) cells [2]. The ICV injection of SB-334867 alone had no effect on the formalin-induced nociceptive behaviors. Pre-treatment with SB-334867 at a dose of 0.5 nmol significantly attenuated the analgesia induced by morphine (at dose 1.5mg/kg of morphine; interphase and phase 2B and at dose 3mg/kg of morphine just phase 2B of formalin test) [3]. Administered alone, SB-334867 (30 mg/kg, but not lower doses) significantly reduced food intake and most active behaviours (eating, grooming, sniffing, locomotion and rearing), while increasing resting. Pretreatment with SB-334867 dose-dependently blocked these effects of orexin-A, with significant antagonism evident at dose levels (3-10 mg/kg) below those required to produce intrinsic behavioural effects under present test conditions in rats [4].Toxicity: Acute systemic treatment with the selective orexin-1 (OX1R) antagonist SB-334867 reduces food intake in rats, an effect associated with an acceleration in behavioural satiety and unrelated to gross behavioural disruption, alterations in palatability, or toxicity.

Related Catalog

Signaling Pathways >>GPCR/G Protein >>Orexin Receptor (OX Receptor)Research Areas >>Neurological Disease

References

[1]. Smart D, et al. SB-334867-A: the first selective orexin-1 receptor antagonist. Br J Pharmacol. 2001 Mar;132(6):1179-82.

[2]. Rasmussen K, et al. The orexin-1 receptor antagonist SB-334867 blocks the effects of antipsychotics on the activity of A9 and A10 dopamine neurons: implications for antipsychotic therapy. Neuropsychopharmacology. 2007 Apr;32(4):786-92.

[3]. Azhdari-Zarmehri H, et al. Orexin receptor type-1 antagonist SB-334867 decreases morphine-induced antinociceptive effect in formalin test. Pharmacol Biochem Behav. 2013 Nov;112:64-70.

[4]. Rodgers RJ, et al. SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats. Eur J Neurosci. 2001 Apr;13(7):1444-52.

Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Boiling Point	549.5±58.0 °C at 760 mmHg
Molecular Formula	C₁₇H₁₃N₅O₂
Molecular Weight	319.317
Flash Point	286.1±32.3 °C
Exact Mass	319.106934
LogP	0.51
Vapour Pressure	0.0±1.5 mmHg at 25°C
Index of Refraction	1.757
Storage condition	-20℃

Safety Information

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315
RIDADR	NONH for all modes of transport

Synonyms

1-(2-Methyl-1,3-benzoxazol-6-yl)-1-(1,5-naphthyridin-4-yl)urea

Urea, N-(2-methyl-6-benzoxazolyl)-N-1,5-naphthyridin-4-yl-

N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl

1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea

SB-334867

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