79689-25-1

79689-25-1 structure

Name: DG5128
Chemical Name: 2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenylethyl]pyridine,dihydrochloride
CAS Number: 79689-25-1
Molecular Formula: C₁₆H₁₉Cl₂N₃
Molecular Weight: 324.24800
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2016-12-12 02:51:42
Modify Date: 2024-01-29 16:32:55
DG5128 is a preferential α2-adrenoceptor antagonist. DG5128 exhibits 7.4 times higher affinity (pKi=6.28) toward α2-adrenoceptor than α1-adrenoceptor.

Name	2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenylethyl]pyridine,dihydrochloride
Synonyms	2-[2-(4,5-dihydro-1h-imidazol-2-yl)-1-phenyl-ethyl]pyridine dihydrochl oride DG5128

Description	DG5128 is a preferential α2-adrenoceptor antagonist. DG5128 exhibits 7.4 times higher affinity (pKi=6.28) toward α2-adrenoceptor than α1-adrenoceptor.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Metabolic Disease
Target	pKi :6.28 (α2-adrenoceptor)[1]
In Vitro	DG5128 (DG-5128) at concentrations up to 10 μM inhibits [3H]clonidine binding more effectively than it doed [3H]prazosin binding in rat cerebral cortex membranes. The mode of inhibition was homogeneous and consistent with the law of simple mass action[1]. The EC50 values for stimulation of insulin release from rat islets and the MIN6 β-cell line induced by DG5128 (Midaglizole) are 200 nM and 24 μM, respectively. The IC50 values for KATP current inhibition induced by DG5128 (Midaglizole) are 3.8 μM and 4.4 uM for Kir6.2 and Kir6.2/SUR1 , respectively[2].
In Vivo	DG5128 (3 and 30 mg/kg, i.v.) increases blood pressure in pithed rats[3].
Animal Admin	Rats[3] Male Wistar rats (290-450 g) are anesthetized with pentobarbital sodium (35 mg/kg, i.p.) and artificially ventilated with room air. Diastolic blood pressure before the administration of the DG5128 (Midaglizole) is about 35 mmHg. DG5128 at doses of 3 and 30 mg/kg produces an increase in blood pressure by 27 and 64 mmHg, respectively, at approximately 1 min after the administration.
References	[1]. Yamanaka K, et al. The selectivity of DG-5128 as an alpha 2-adrenoceptor antagonist. Eur J Pharmacol. 1984 Nov 27;106(3):625-8. [2]. Proks P, et al. Inhibition of recombinant K(ATP) channels by the antidiabetic agents midaglizole, LY397364 and LY389382. Eur J Pharmacol. 2002 Sep 27;452(1):11-9. [3]. Hirohashi M, et al. Intrinsic pressor activity of midaglizole, an alpha-2 adrenoceptor antagonist, in pithed rats. Jpn J Pharmacol. 1990 Aug;53(4):519-20.

Boiling Point	460ºC at 760 mmHg
Molecular Formula	C₁₆H₁₉Cl₂N₃
Molecular Weight	324.24800
Flash Point	232ºC
Exact Mass	323.09600
PSA	37.28000
LogP	3.97370

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