498-96-4 Usage
Description
Guvacine Hydrochloride is an alpha, beta-unsaturated monocarboxylic acid derived from nicotinic acid, which has been hydrogenated at the 1-2 and 5-6 positions of the pyridine ring. It functions as a GABA uptake inhibitor, targeting various GABA transporters such as hGABA T-1, rGABA T-2, hGABA T-3, and hBGT-1. GABA, or Gamma-Aminobutyric acid, is the primary inhibitory neurotransmitter in the mammalian brain, making Guvacine Hydrochloride a potential candidate for treating neuropsychiatric disorders.
Uses
Used in Pharmaceutical Industry:
Guvacine Hydrochloride is used as a GABA uptake inhibitor for its potential role in treating neuropsychiatric disorders. By inhibiting the reuptake of GABA, it can help maintain higher levels of this neurotransmitter in the brain, which may contribute to the alleviation of symptoms associated with these disorders.
Used in Neurochemistry Research:
In the field of neurochemistry, Guvacine Hydrochloride is used as a research tool to study the function and regulation of GABA transporters. Understanding the interactions between Guvacine Hydrochloride and these transporters can provide valuable insights into the mechanisms underlying various neuropsychiatric conditions and guide the development of novel therapeutic strategies.
Biological Activity
Specific GABA uptake inhibitor. IC 50 values are 14, 58, 119 and 1870 mM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively.
Check Digit Verification of cas no
The CAS Registry Mumber 498-96-4 includes 6 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 3 digits, 4,9 and 8 respectively; the second part has 2 digits, 9 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 498-96:
(5*4)+(4*9)+(3*8)+(2*9)+(1*6)=104
104 % 10 = 4
So 498-96-4 is a valid CAS Registry Number.
InChI:InChI=1/C6H9NO2/c8-6(9)5-2-1-3-7-4-5/h2,7H,1,3-4H2,(H,8,9)
498-96-4Relevant articles and documents
Discovery of potent iminoheterocycle BACE1 inhibitors
Caldwell, John P.,Mazzola, Robert D.,Durkin, James,Chen, Joseph,Chen, Xia,Favreau, Leonard,Kennedy, Matthew,Kuvelkar, Reshma,Lee, Julie,McHugh, Nansie,McKittrick, Brian,Orth, Peter,Stamford, Andrew,Strickland, Corey,Voigt, Johannes,Wang, Liyang,Zhang, Lili,Zhang, Qi,Zhu, Zhaoning
, p. 5455 - 5459 (2015/01/08)
The synthesis of a series of iminoheterocycles and their structure-activity relationships (SAR) as inhibitors of the aspartyl protease BACE1 will be detailed. An effort to access the S3 subsite directly from the S1 subsite initially yielded compounds with sub-micromolar potency. A subset of compounds from this effort unexpectedly occupied a different binding site and displayed excellent BACE1 affinities. Select compounds from this subset acutely lowered Aβ40 levels upon subcutaneous and oral administration to rats.
USE OF NEUROPROTECTIVE COMPOUNDS IN OBTAINING MEDICAMENTS INTENDED FOR THE TREATMENT OF NEURODEGENERATING DISEASES
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, (2009/12/23)
Use of neuroprotective compounds in obtaining medicaments intended for the curative treatment of neurodegenerative disease and/or the prevention of the appearance of disorders ensuing from those diseases.
Inhibitors of GABA uptake. Syntheses and 1H NMR spectroscopic investigations of guvacine, (3RS,4SR)-4-hydroxypiperidine-3-carboxylic acid, and related compounds
Krogsgaard-Larsen,Thyssen,Schaumburg
, p. 327 - 334 (2007/10/04)
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