product name Medetomidine HCl
Description: Medetomidine HCl, also known as MPV-785, is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, it exhibits 1620-fold selectivity over α1-adrenoceptor. Medetomidine is a synthetic drug used as both a surgical anesthetic and analgesic. It is an alpha-2 adrenergic agonist that can be administered as an intravenous drug solution with sterile water. Medetomidine is a racemic mixture of two stereoisomers; dexmedetomidine is the isomer with more useful effects, and is now marketed as Dexdomitor.
References: Eur J Pharmacol. 1988 May 20;150(1-2):9-14; J Auton Pharmacol. 1986 Dec;6(4):275-84.
236.74
Formula
C13H16N2.HCl
CAS No.
86347-15-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 12 mg/mL (50.7 mM)
Water: 47 mg/mL (198.5 mM)
Ethanol: 47 mg/mL (198.5 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19398680
| In Vitro |
In vitro activity: Medetomidine is a selectiveα2-adrenoceptor agonist, with Ki of 1.08 nM, exhibits 1620-fold selectivity over α1-adrenoceptor, has very weak or no binding to other neurotransmitter receptors. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In anesthetized rats, medetomidine (1-100 μg/kg, i.v.) induces a dose-dependent, relatively short-lived reduction in blood pressure and heart rate. In the pithed rat, medetomidine shows very potent vasopressor (PD50 1.7 μg/kg) and sympatho-inhibitory (ID50 1.6 μg/kg) effects without affecting basal heart rate. Medetomidine induces dose-dependent sedation, which at high doses (>100μg/kg) includes loss of the righting reflex and hypothermia. Medetomidine induces a decreases in the turnover rate of biogenic amines in the brain, dose-dependently inhibits norepinephrine (NE) turnover, inhibits brain dopamine turnover at high doses, decreases serotonin turnover. |
| Animal model | Rat |
| Formulation & Dosage | Dissolved in saline; 1-100 μg/kg; i.v. injection |
| References | Eur J Pharmacol. 1988 May 20;150(1-2):9-14; J Auton Pharmacol. 1986 Dec;6(4):275-84. |
Related Posts
product name Medetomidine HCl
Description: Medetomidine HCl, also known as MPV-785, is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, it exhibits 1620-fold selectivity over α1-adrenoceptor. Medetomidine is a synthetic drug used as both a surgical anesthetic and analgesic. It is an alpha-2 adrenergic agonist that can be administered as an intravenous drug solution with sterile water. Medetomidine is a racemic mixture of two stereoisomers; dexmedetomidine is the isomer with more useful effects, and is now marketed as Dexdomitor.
References: Eur J Pharmacol. 1988 May 20;150(1-2):9-14; J Auton Pharmacol. 1986 Dec;6(4):275-84.
236.74
Formula
C13H16N2.HCl
CAS No.
86347-15-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 12 mg/mL (50.7 mM)
Water: 47 mg/mL (198.5 mM)
Ethanol: 47 mg/mL (198.5 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19398680
| In Vitro |
In vitro activity: Medetomidine is a selectiveα2-adrenoceptor agonist, with Ki of 1.08 nM, exhibits 1620-fold selectivity over α1-adrenoceptor, has very weak or no binding to other neurotransmitter receptors. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In anesthetized rats, medetomidine (1-100 μg/kg, i.v.) induces a dose-dependent, relatively short-lived reduction in blood pressure and heart rate. In the pithed rat, medetomidine shows very potent vasopressor (PD50 1.7 μg/kg) and sympatho-inhibitory (ID50 1.6 μg/kg) effects without affecting basal heart rate. Medetomidine induces dose-dependent sedation, which at high doses (>100μg/kg) includes loss of the righting reflex and hypothermia. Medetomidine induces a decreases in the turnover rate of biogenic amines in the brain, dose-dependently inhibits norepinephrine (NE) turnover, inhibits brain dopamine turnover at high doses, decreases serotonin turnover. |
| Animal model | Rat |
| Formulation & Dosage | Dissolved in saline; 1-100 μg/kg; i.v. injection |
| References | Eur J Pharmacol. 1988 May 20;150(1-2):9-14; J Auton Pharmacol. 1986 Dec;6(4):275-84. |