927691-21-2 Usage
Description
(R)-6,7-dimethoxy-4-(3-(quinoxalin-2-yloxy)pyrrolidin-1-yl)quinazoline, also known as PQ-10, is a potent and selective inhibitor of phosphodiesterase type 10 (PDE10) with a Ki value of 4 nM. It exhibits high selectivity for PDE10 over a panel of 60 CNS-associated receptors, enzymes, and ion channels in vitro. PQ-10 has been shown to increase striatal cGMP and phosphorylation of cAMP response element binding protein (CREB) in murine striatum, which are known markers of in vivo PDE10 inhibition. Additionally, PQ-10 has demonstrated the ability to reduce memory deficits induced by scopolamine and MK-801 in rats. It also exhibits anti-tumor activity with IC50 values of 0.29 and 0.22 mM for HCT116 and SW480 colon cancer cells, respectively.
Uses
Used in Pharmaceutical Industry:
PQ-10 is used as a potent and selective inhibitor of PDE10 for the treatment of various central nervous system (CNS) disorders. Its high selectivity for PDE10 over other CNS-associated receptors, enzymes, and ion channels makes it a promising candidate for the development of targeted therapies.
Used in Memory Enhancement Applications:
PQ-10 is used as a memory-enhancing agent for the treatment of memory deficits induced by scopolamine and MK-801 in rats. Its ability to increase striatal cGMP and phosphorylation of CREB in murine striatum suggests its potential in improving cognitive function and memory.
Used in Anticancer Applications:
PQ-10 is used as an anticancer agent for the inhibition of tumor cell growth in HCT116 and SW480 colon cancer cells. Its IC50 values of 0.29 and 0.22 mM, respectively, indicate its potential as a therapeutic agent for the treatment of colon cancer.
Used in Drug Development Research:
PQ-10 is used as a research tool for the investigation of PDE10 inhibition and its effects on various biological processes. Its high selectivity and potency make it a valuable compound for studying the role of PDE10 in CNS disorders and other diseases.
Biochem/physiol Actions
PQ-10 is a potent and selective inhibitor of phosphodiesterase 10A (PDE10). Apparently, PQ-10 enhances basic auditory information processing in rats. PQ-10 as other PED10 inhibitors suppresses a growth of human non-small cell lung cancer (NSCLC) cell lines.
Check Digit Verification of cas no
The CAS Registry Mumber 927691-21-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,2,7,6,9 and 1 respectively; the second part has 2 digits, 2 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 927691-21:
(8*9)+(7*2)+(6*7)+(5*6)+(4*9)+(3*1)+(2*2)+(1*1)=202
202 % 10 = 2
So 927691-21-2 is a valid CAS Registry Number.
927691-21-2Relevant articles and documents
TREATMENT AND DIAGNOSIS OF CANCER AND PRECANCEROUS CONDITIONS USING PDE10A INHIBITORS AND METHODS TO MEASURE PDE10A EXPRESSION
-
Paragraph 0132, (2015/02/02)
Disclosed are methods for treating cancer and precancerous conditions with PDE10A specific inhibitors and diagnosis of neoplastic diseases based on elevated levels of PDE10A.
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors
Chappie, Thomas A.,Humphrey, John M.,Allen, Martin P.,Estep, Kimberly G.,Fox, Carol B.,Lebel, Lorraine A.,Liras, Spiros,Marr, Eric S.,Menniti, Frank S.,Pandit, Jayvardhan,Schmidt, Christopher J.,Tu, Meihua,Williams, Robert D.,Yang, Feng V.
, p. 182 - 185 (2007/10/03)
A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal
PHOSPHODIESTERASE 10 INHIBITION AS TREATMENT FOR OBESITY-RELATED AND METABOLIC SYNDROME-RELATED CONDITIONS
-
Page/Page column 20, (2008/06/13)
The present invention provides methods to decrease body weight and/or body fat in animals, e.g., in the treatment of overweight or obese patients (e.g., humans or companion animals), or as a means to produce leaner meat in food stock animals (e.g., cattle, chickens, pigs), methods to treat non-insulin dependent diabetes (NIDDM), metabolic syndrome, or glucose intolerance, in patients in need thereof by administering a PDE10 inhibitor (alone or in combination with another therapeutic agent), kits for the above-identified therapeutic uses, and methods of identifying PDE10 inhibitors for the above-described therapeutic uses.
