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113775-47-6

113775-47-6 structure
113775-47-6 structure
  • Name: Dexmedetomidine
  • Chemical Name: dexmedetomidine
  • CAS Number: 113775-47-6
  • Molecular Formula: C13H16N2
  • Molecular Weight: 200.28000
  • Catalog: Biochemical Inhibitor Neuronal Signaling Adrenergic Receptor Agonist
  • Create Date: 2018-05-10 08:00:00
  • Modify Date: 2024-01-05 00:07:03
  • Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].

Name dexmedetomidine
Synonyms Dexmedetomidine
5-[(1S)-1-(2,3-dimethylphenyl)ethyl]-1H-imidazole
Dexmedetomidina
(S)-medetomidine
Dexmedetomidinum
1H-Imidazole,5-[(1S)-1-(2,3-dimethylphenyl)ethyl]-
Description Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
Related Catalog
Target

α2-adrenergic receptor:1.08 nM (Ki)

In Vitro Medetomidine has high selectivity for α2 adrenoceptors (Ki=1.08 nM) over α1 adrenoceptors (Ki=1750 nM) in rat brain membranes as measured by the displacement of [3H]clonidine[1]. Medetomidine (0.1-100 nM) inhibits the twitch response in field-stimulated mouse vas deferens, with a pD2 of 9.0[1].
In Vivo Medetomidine (10-100 μg/kg; i.v. at 5-min intervals) produces a dose-dependent pupillary dilatation in pentobarbitone-anaesthetized rats[1]. Animal Model: Female Sprague-Dawley rats (270-350 g)[1] Dosage: 1, 5, 10, 50, 100 mg/kg Administration: I.v. at 5-min intervals Result: Produced the pupil dilatation of 2.5 mm (approximately half of the maximum effect) at the cumulative dose of 4 μg/kg.
References

[1]. Virtanen R, et, al. Characterization of the selectivity, specificity and potency of medetomidine as an alpha 2-adrenoceptor agonist. Eur J Pharmacol. 1988 May 20;150(1-2):9-14.

[2]. Gertler R, et, al. Dexmedetomidine: a novel sedative-analgesic agent. Proc (Bayl Univ Med Cent). 2001 Jan;14(1):13-21.

[3]. Sajid B, et, al. A comparison of oral dexmedetomidine and oral midazolam as premedicants in children. J Anaesthesiol Clin Pharmacol. Jan-Mar 2019;35(1):36-40.

Density 1.053g/cm3
Boiling Point 381.9ºC at 760mmHg
Melting Point 146-149°C
Molecular Formula C13H16N2
Molecular Weight 200.28000
Flash Point 191.3ºC
Exact Mass 200.13100
PSA 28.68000
LogP 3.17830
Vapour Pressure 1.08E-05mmHg at 25°C
Index of Refraction 1.569
Storage condition 2-8°C
HS Code 2933290090

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113775-47-6 structure

113775-47-6

Literature: NEON LABORATORIES LTD.; DALVI, Mahesh Bhagoji; KENNY, Rajesh Shashikant; TARADE, Pradeep Kisan Patent: WO2013/69025 A1, 2013 ; Location in patent: Page/Page column 7 ;

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113775-47-6 structure

113775-47-6

Literature: Synthetic Communications, , vol. 26, # 8 p. 1585 - 1593

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113775-47-6 structure

113775-47-6

Literature: Synthetic Communications, , vol. 26, # 8 p. 1585 - 1593

~%

113775-47-6 structure

113775-47-6

Literature: Synthetic Communications, , vol. 26, # 8 p. 1585 - 1593

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113775-47-6 structure

113775-47-6

Literature: Synthetic Communications, , vol. 26, # 8 p. 1585 - 1593
Precursor  4

DownStream  0

HS Code 2933290090
Summary 2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%