DEXMEDETOMIDINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C13H16N2
Molecular Weight	200.2795
Optical Activity	( + )
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

C[C@H](C1=CN=CN1)C2=CC=CC(C)=C2C

InChI

InChIKey=CUHVIMMYOGQXCV-NSHDSACASA-N

InChI=1S/C13H16N2/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13/h4-8,11H,1-3H3,(H,14,15)/t11-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C13H16N2
Molecular Weight	200.2795
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description

Dexmedetomide (biologically active dextroisomer of medetomidine) is an alpha2-adrenergic agonist which was approved by FDA for the sedation purposes. Upon administration the drug activates the alpha2 receptors thus inhibiting the release of norepinephrine and terminating the propagation of pain signals. Also it inhibits sympathetic activity and thus can decrease blood pressure and heart rate.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Adrenergic receptor alpha-2 114	Agonist 2,752

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pain 619	Preventing		Approved 8,583	PRECEDEX

C_max

Value	Dose	Co-administered	Analyte	Population
2.6 ng/mL	1 μg/kg bw single, intravenous		DEXMEDETOMIDINE plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
107.58 ng × h/mL	1 μg/kg bw single, intravenous		DEXMEDETOMIDINE plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
138 min	1 μg/kg bw single, intravenous		DEXMEDETOMIDINE plasma	Homo sapiens

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:4466	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:4466
ChemicalBook	CB41017166	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB41017166
MolPort	MolPort-035-395-718	https://www.molport.com/shop/molecule-link/MolPort-035-395-718
Selleck Chemicals	dexmedetomidine	http://www.selleckchem.com/products/dexmedetomidine.html
ZINC	ZINC000004632106	http://zinc15.docking.org/substances/ZINC000004632106

Showing 1 to 5 of 5 entries

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PubMed

Show entries

Title	Date	PubMed
Preliminary UK experience of dexmedetomidine, a novel agent for postoperative sedation in the intensive care unit.	1999 Dec	10594409
Characterization of human recombinant alpha(2A)-adrenoceptors expressed in Chinese hamster lung cells using intracellular Ca(2+) changes: evidence for cross-talk between recombinant alpha(2A)- and native alpha(1)-adrenoceptors.	2000 Apr	10742289
Noradrenergic regulation of hippocampal place cells.	2001	11811674
[Efficacy of oncologic surgery. Does anesthesia influence the postoperative outcome?].	2001 Apr	11370395
Contribution of alpha(2) receptor subtypes to nerve injury-induced pain and its regulation by dexmedetomidine.	2001 Apr	11309255

Showing 1 to 5 of 35 entries

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Patents

Sample Use Guides

In Vivo Use Guide

For Adult Intensive Care Unit Sedation: Generally initiate at one mcg/kg over 10 minutes, followed by a maintenance infusion of 0.2 to 0.7 mcg/kg/hour. For Adult Procedural Sedation: Generally initiate at one mcg/kg over 10 minutes, followed by a maintenance infusion initiated at 0.6 mcg/kg/hour and titrated to achieve desired clinical effect with doses ranging from 0.2 to 1 mcg/kg/hour.

Route of Administration: Intravenous

In Vitro Use Guide

Strips of pregnant human myometrium obtained from six individuals at elective caesarean section were incubated with dexmedetomidine (1x10(-11) to 1x10(-6) g/mL) and the in vitro effect was studied as the drug may be used in obstetric anaesthesia