92564-08-4
Chemical Structure
HA-1004 dihydrochloride
- CAS No.: 92564-08-4
- Formula:C12H17Cl2N5O2S
- Molecular Weight:366.27
IUPAC Name: N-(2-guanidinoethyl)isoquinoline-5-sulfonamide dihydrochloride
InChIKey: PMTUBVLLVFJRLK-UHFFFAOYSA-N
SMILES: O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC(N)=N)=O.[H]Cl.[H]Cl
Biological Activity: HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models[1][2][3].
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HA-1004 dihydrochloride | HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models. | |||||||||||||||||||||
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References
- [1]. Almela P, et al. Crosstalk between G protein-coupled receptors (GPCRs) and tyrosine kinase receptor (TXR) in the heart after morphine withdrawal. Front Pharmacol. 2013 Dec 27;4:164. [Content Brief]
- [2]. Goodman HM, et al. The isoquinoline sulfonamide inhibitors of protein phosphorylation, H-7, H-8, and HA-1004, also inhibit RNA synthesis: studies on responses of adipose tissue to growth hormone. Endocrinology. 1990 Jan;126(1):441-50. [Content Brief]
- [3]. Ishikawa T, et al. Relaxation of vascular smooth muscle by HA-1004, an inhibitor of cyclic nucleotide-dependent protein kinase. J Pharmacol Exp Ther. 1985 Nov;235(2):495-9. [Content Brief]
