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BUPRENORPHINE

BUPRENORPHINE
BUPRENORPHINE structure
CAS No.
52485-79-7
Chemical Name:
BUPRENORPHINE
Synonyms
UM-952;Lepetan;rx6029m;Subutex;Temgesi;Buprenex;NIH-8805;Temgesic;CL-112302;Buprenorfin
CBNumber:
CB0279103
Molecular Formula:
C29H41NO4.ClH
Formula Weight:
504.11
MOL File:
52485-79-7.mol

BUPRENORPHINE Properties

Melting point:
260-262°C
Boiling point:
570.1°C (rough estimate)
Density 
1.0953 (rough estimate)
refractive index 
1.6290 (estimate)
Flash point:
9℃
storage temp. 
?20°C
solubility 
Very slightly soluble in water, freely soluble in acetone, soluble in methanol, slightly soluble in cyclohexane. It dissolves in dilute solutions of acids.
pka
pKa 8.24(H2O t=23.0±0.3) (Uncertain)
CAS DataBase Reference
52485-79-7
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  F,T
Risk Statements  11-23/24/25-39/23/24/25
Safety Statements  16-36/37-45-7
RIDADR  UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany  1
Symbol(GHS):
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H225 Highly Flammable liquid and vapour Flammable liquids Category 2 Danger P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H370 Causes damage to organs Specific target organ toxicity, single exposure Category 1 Danger P260, P264, P270, P307+P311, P321,P405, P501
Precautionary statements:
P210 Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P260 Do not breathe dust/fume/gas/mist/vapours/spray.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P311 Call a POISON CENTER or doctor/physician.
P301+P310 IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

BUPRENORPHINE price

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BUPRENORPHINE Chemical Properties,Uses,Production

Chemical Properties

White Solid

Uses

Controllled substance (narcotic). Analgesic that demonstrates narcotic agonist-antagonist properties.

Definition

ChEBI: A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is su stituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group.

brand name

Buprenex (Reckitt Benckiser); Subutex (Reckitt Benckiser);Buprex;Buprx;Finibron;Prefin;Temagesic.

World Health Organization (WHO)

Buprenorphine, an opioid analgesic with both morphine agonist and antagonist activity, was introduced in 1978. It was originally considered to possess low dependence potential. However, it has latterly been identified as causing a socially significant abuse problem in several countries which have consequently subjected it to control in 1989 under Schedule III of the 1971 Convention of Psychotropic Substances. (Reference: (UNCPS3) United Nations Convention on Psychotropic Substances (III), , , 1971)

General Description

Buprenorphine is a semisynthetic, highly lipophilic opiate derivedfrom thebaine. Pharmacologically, it is classified as amixed μ-agonist/antagonist (a partial agonist) and a weak κ-antagonist. It has a high affinity for the μ-receptors(1,000 times greater than morphine) and a slow dissociationrate leading to its long duration of action (6–8 hours). Atrecommended doses, it acts as an agonist at the μ-receptorwith approximately 0.3 mg IV equianalgesic to 10 mg of IVmorphine. One study in humans found that buprenorphine displaysa ceiling effect to the respiratory depression, but not theanalgesic effect over a dose range of 0.05 to 0.6 mg.In practice,this makes buprenorphine a safer opiate (when usedalone) than pure μ-agonists. Relatively few deaths frombuprenorphine overdose (when used alone) have been reported.113 The tight binding of the drug to the receptor also hasled to mixed reports on the effectiveness of using naloxone toreverse the respiratory depression. In animal studies, normaldoses of the pure antagonist naloxone were unable to removebuprenorphine from the receptor site and precipitate withdrawal.In a human study designed to precipitate withdrawalfrom buprenorphine, a naloxone dose (mean=35 mg) 100times the dose usually needed to precipitate withdrawal inmethadone-dependent subjects was used. For comparison, approximately0.3 mg, 4 mg, 4 mg, and 10 mg of naloxonewould be required to precipitate withdrawal from heroin, butorphanol,nalbuphine, or pentazocine respectively.

Contact allergens

This semisynthetic opioid analgesic drug is derived fromwith transdermal systems (TDS). In case of localized or generalized allergic contact dermatitis due to buprenorphine in TDS, TDS containing fentanyl can be safely used thebaine. It can be used parenterally, orally, and topically

BUPRENORPHINE Preparation Products And Raw materials

Raw materials

Preparation Products


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