Alvimopan

Modify Date: 2024-01-02 10:19:35

Alvimopan structure	Common Name	Alvimopan
	CAS Number	156053-89-3	Molecular Weight	424.533
	Density	1.2±0.1 g/cm3	Boiling Point	684.1±55.0 °C at 760 mmHg
	Molecular Formula	C₂₅H₃₂N₂O₄	Melting Point	210-213ºC
	MSDS	Chinese USA	Flash Point	367.5±31.5 °C
	Symbol	GHS07, GHS09	Signal Word	Warning

Use of Alvimopan

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. IC50 Value: 1.7 nM (Mu-type opioid receptor) [1]Target: mu-opioid receptorin vitro: The dissociation rate of alvimopan from the micro opioid receptor (t(1/2)=30--44 min) was comparable to that of the long acting partial agonist buprenorphine (t(1/2)=44 min), but was slower than those of the antagonists naloxone (t(1/2)=0.82 min) and N-methylnaltrexone (t(1/2)=0.46 min) [2].in vivo: Alvimopan did not significantly accelerate GI-3 compared with placebo [6 mg: hazard ratio (HR) = 1.20, p = 0.080; 12 mg: HR = 1.24, p = 0.038). However, after adjustment for significant covariates (sex/surgical duration), benefits were significant for both doses (6 mg: HR = 1.24, p = 0.037; 12 mg: HR = 1.26, p = 0.028). Alvimopan also significantly accelerated time to GI-2 (6 mg: HR = 1.37, p = 0.008; 12 mg: HR = 1.33, p = 0.018) and DCO (6 mg: HR = 1.31, p = 0.008; 12 mg: HR = 1.28, p = 0.015) [3]. Alvimopan (1 and 3 mg/kg) significantly reversed this delayed GI transit when administered 45 min prior to surgery. However, the effects of alvimopan were less pronounced when administered following surgery [4].Toxicity:The most common treatment-emergent adverse events across all treatment groups were nausea, vomiting, and hypotension; the incidence of nausea and vomiting was reduced by 53 percent in thealvimopan 12-mg group [5].Clinical trial: Intercostal Nerve Block With Liposome Bupivacaine in Subjects Undergoing Posterolateral Thoracotomy. Phase 3

Name	Alvimopan
Synonym	More Synonyms

Description	Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. IC50 Value: 1.7 nM (Mu-type opioid receptor) [1]Target: mu-opioid receptorin vitro: The dissociation rate of alvimopan from the micro opioid receptor (t(1/2)=30--44 min) was comparable to that of the long acting partial agonist buprenorphine (t(1/2)=44 min), but was slower than those of the antagonists naloxone (t(1/2)=0.82 min) and N-methylnaltrexone (t(1/2)=0.46 min) [2].in vivo: Alvimopan did not significantly accelerate GI-3 compared with placebo [6 mg: hazard ratio (HR) = 1.20, p = 0.080; 12 mg: HR = 1.24, p = 0.038). However, after adjustment for significant covariates (sex/surgical duration), benefits were significant for both doses (6 mg: HR = 1.24, p = 0.037; 12 mg: HR = 1.26, p = 0.028). Alvimopan also significantly accelerated time to GI-2 (6 mg: HR = 1.37, p = 0.008; 12 mg: HR = 1.33, p = 0.018) and DCO (6 mg: HR = 1.31, p = 0.008; 12 mg: HR = 1.28, p = 0.015) [3]. Alvimopan (1 and 3 mg/kg) significantly reversed this delayed GI transit when administered 45 min prior to surgery. However, the effects of alvimopan were less pronounced when administered following surgery [4].Toxicity:The most common treatment-emergent adverse events across all treatment groups were nausea, vomiting, and hypotension; the incidence of nausea and vomiting was reduced by 53 percent in thealvimopan 12-mg group [5].Clinical trial: Intercostal Nerve Block With Liposome Bupivacaine in Subjects Undergoing Posterolateral Thoracotomy. Phase 3
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Metabolic Disease
References	[1]. NCBI BioAssay: 325959 [2]. Cassel JA, et al. [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol. 2005 Sep 27;520(1-3):29-36. [3]. Viscusi ER, et al. Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study. Surg Endosc. 2006 Jan;20(1):64-70. [4]. Fukuda H, et al. The selective mu opioid receptor antagonist, alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res. 2006 Aug 2;1102(1):63-70. [5]. Delaney CP, et al. Phase III trial of alvimopan, a novel, peripherally acting, mu opioid antagonist, for postoperative ileus after major abdominal surgery. Dis Colon Rectum. 2005 Jun;48(6):1114-25; discussion 1125-6; author reply 1127-9.

Description

Related Catalog

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor

Signaling Pathways >> Neuronal Signaling >> Opioid Receptor

Research Areas >> Metabolic Disease

References

[1]. NCBI BioAssay: 325959

[2]. Cassel JA, et al. [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol. 2005 Sep 27;520(1-3):29-36.

[3]. Viscusi ER, et al. Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study. Surg Endosc. 2006 Jan;20(1):64-70.

[4]. Fukuda H, et al. The selective mu opioid receptor antagonist, alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res. 2006 Aug 2;1102(1):63-70.

[5]. Delaney CP, et al. Phase III trial of alvimopan, a novel, peripherally acting, mu opioid antagonist, for postoperative ileus after major abdominal surgery. Dis Colon Rectum. 2005 Jun;48(6):1114-25; discussion 1125-6; author reply 1127-9.

Density	1.2±0.1 g/cm3
Boiling Point	684.1±55.0 °C at 760 mmHg
Melting Point	210-213ºC
Molecular Formula	C₂₅H₃₂N₂O₄
Molecular Weight	424.533
Flash Point	367.5±31.5 °C
Exact Mass	424.236206
PSA	89.87000
LogP	3.38
Vapour Pressure	0.0±2.2 mmHg at 25°C
Index of Refraction	1.572
Storage condition	2-8°C

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H315-H319-H400
Precautionary Statements	P273-P280-P305 + P351 + P338-P337 + P313-P391
RIDADR	UN 3077 9 / PGIII
HS Code	2933399090

N/A

CAS#:145603-86-7

Alvimopan

CAS#:156053-89-3

Literature: Zimmerman, Dennis M.; Gidda, Jaswant S.; Cantrell, Buddy E.; Schoepp, Darryle D.; Johnson, Bryan G.; Leander, J. David Journal of Medicinal Chemistry, 1994 , vol. 37, # 15 p. 2262 - 2265

ethyl 2-benzyla...

CAS#:20593-63-9

Alvimopan

CAS#:156053-89-3

Literature: Journal of Medicinal Chemistry, , vol. 37, # 15 p. 2262 - 2265

(+)-(3R,4R)-3,4...

CAS#:119193-19-0

Alvimopan

CAS#:156053-89-3

Literature: Journal of Medicinal Chemistry, , vol. 37, # 15 p. 2262 - 2265

Benzenepropanoi...

CAS#:147383-72-0

Alvimopan

CAS#:156053-89-3

Literature: WO2011/161646 A2, ;

Glycine, N-[(2S...

CAS#:1314751-83-1

Alvimopan

CAS#:156053-89-3

Literature: WO2011/161646 A2, ;

Precursor 3
CAS#:20593-63-9 ethyl 2-benzyla... CAS#:119193-19-0 (+)-(3R,4R)-3,4... CAS#:147383-72-0 Benzenepropanoi...
DownStream 0

HS Code	2933399090
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Alvimopan

N-{(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl}glycine

Glycine, N-[(2S)-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]-1-oxo-2-(phenylmethyl)propyl]-

N-{(2S)-2-Benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]propanoyl}glycine

Unii-Q153V49p3z

DC Chemicals Limited
China
Product Name: AlviMopan
Price: $450.0/100mg $800.0/250mg $1700.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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Alvimopan

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