EPTAZOCINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C15H21NO
Molecular Weight	231.3333
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12CC3=C(C=C(O)C=C3)[C@@](C)(C1)CCN(C)C2

InChI

InChIKey=ZOWQTJXNFTWSCS-IAQYHMDHSA-N

InChI=1S/C15H21NO/c1-15-5-6-16(2)10-11(9-15)7-12-3-4-13(17)8-14(12)15/h3-4,8,11,17H,5-7,9-10H2,1-2H3/t11-,15-/m1/s1

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Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/15278579

Eptazocine is an opioid analgesic which was introduced in 1987 by Morishita in Japan . It acts as a mixed κappa opioid receptor agonist and mu-opioid receptor antagonist.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Mu opioid receptor 221 Target ID: CHEMBL233 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2992058	Antagonist 2778
Kappa opioid receptor 108 Target ID: CHEMBL237 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2992058	Agonist 2678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pain 614 Sources: http://link.springer.com/article/10.1007/BF03305983?view=classic	Primary		Approved 8429	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
The interaction of eptazocine, a novel analgesic, with opioid receptors.	1985 May	2992058
[Preferential action of eptazocine, a novel analgesic, with opioid receptors in isolated guinea pig ileum and mouse vas deferens preparations].	1990 Jan	2154395

Patents

Sample Use Guides

In Vivo Use Guide

The induction of anesthesia was started with eptazocine 30 mg iv and thiopental 3-4 mg.kg-1 iv and the trachea was intubated smoothly following succinylcholine 40 mg iv. Then, they were given intravenous droperidol 0.15 mg.kg-1 with inhalation of 70% N2O and 30% O2. Good intraoperative muscle relaxation was obtained by dialferine or pancuronium.

Route of Administration: Intravenous

In Vitro Use Guide

Eptazocine caused a concentration-dependent inhibition against the [3H]-naloxone [( 3H]-NLX) specific binding to rat brain synaptic membrane in the absence of sodium cation and GTP (IC50; 7.83 +/- 1.57 microM). The ratios of IC50 values between the absence to the presence of sodium cation alone or sodium cation and GTP were 3.89 and 4.35, respectively. In addition, eptazocine (10 microM) also produced the significant decrease of [3H]-NLX specific binding in the mouse brain synaptic membrane

Name

Type

Language

EPTAZOCINE

Official Name

English

eptazocine [INN]

Common Name

English

Eptazocine [WHO-DD]

Common Name

English

(-)-(1S,6S)-2,3,4,5,6,7-HEXAHYDRO-1,4-DIMETHYL-1,6-METHANO-1H-4-BENZAZONIN-10-OL

Systematic Name

English

EPTAZOCINE [MI]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C241