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Desglymidodrine

Names

[ CAS No. ]:
3600-87-1

[ Name ]:
Desglymidodrine

[Synonym ]:
Midodrine Related Compound A
ST 1059 (Desglymidodrine)
2-amino-1-(2,5-dimethoxyphenyl)ethan-1-ol
(+/-)-2-amino-1-(2,5-dimethoxyphenyl)ethanol
1-(2',5'-Dimethoxyphenyl)aminoethanol
1-(2',5'-dimethoxyphenyl)-2-aminoethanol
de-glymidodrine

Biological Activity

[Description]:

Desglymidodrine (ST 1059), the active metabolite of midodrine, is a selective α1-adrenoceptor agonist. Desglymidodrine is an effective arterial and venous vasoconstrictor and can be used to regulate blood pressure[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[Target]

α1A-adrenergic receptor:5.89 (pKi)

α1B-adrenergic receptor:5.16 (pKi)

rat alpha1D-adrenergic receptor:5.78 (pKi)

human α2A-adrenoceptor:5.83 (pKi)


[In Vitro]

Desglymidodrine (ST 1059) (1-1000 μM) affects vein contraction with the pD2 values (negative logarithm of the concentration which causes 50% of the maximum possible effect) of 4.64 (- log mol/L) in dog isolated femoral veins and 4.48 (- log mol/L) in isolated human saphenous veins, respectively[1]. Desglymidodrine (ST 1059) acts on α1A, α1B, α1D in rat and α2A in human adrenoceptor with the pKi values of 5.89, 5.16, 5.78 and 5.83, respectively[2].

[References]

[1]. K Nakayama, et al. Effects of anisotropine methylbromide (Valpin) and its mixture with sulpyrine on vocalization response and spasm of intestine induced by acetylcholine in dogs. Jpn J Pharmacol. 1972 Apr;22(2):215-20.

[2]. Steven ABuckner, et al. ABT-866, a novel α1A-adrenoceptor agonist with antagonist properties at the α1B- and α1D-adrenoceptor subtypes,European Journal of Pharmacology,Volume 449, Issues 1–2,2002,Pages 159-1

Chemical & Physical Properties

[ Boiling Point ]:
364.3ºC at 760mmHg

[ Melting Point ]:
146-150ºC dec.

[ Molecular Formula ]:
C10H15NO3

[ Molecular Weight ]:
197.23100

[ Flash Point ]:
174.1ºC

[ Exact Mass ]:
197.10500

[ PSA ]:
64.71000

[ LogP ]:
1.39620

[ Index of Refraction ]:
1.542

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xn

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2922509090

Precursor & DownStream

Customs

[ HS Code ]: 2922509090

[ Summary ]:
2922509090. other amino-alcohol-phenols, amino-acid-phenols and other amino-compounds with oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%


Related Compounds