101303-98-4 Usage
Description
Zacopride hydrochloride is a pharmaceutical compound that acts as a highly potent SR-3 antagonist and SR-4 agonist. It is also recognized as a 5-HT3 receptor antagonist, which plays a significant role in its various applications. Zacopride hydrochloride has the ability to activate IK1 channels, which are crucial for certain physiological processes.
Uses
Used in Pharmaceutical Industry:
Zacopride hydrochloride is used as a therapeutic agent for treating various conditions related to the central nervous system. Its role as a 5-HT3 receptor antagonist makes it a potential candidate for managing nausea and vomiting associated with chemotherapy, as well as other gastrointestinal disorders.
Used in Research and Development:
In the field of research, Zacopride hydrochloride is utilized as a valuable tool for studying the functions and interactions of the 5-HT3 receptor. Its antagonistic properties allow scientists to investigate the receptor's role in various physiological and pathological processes, leading to a better understanding of its potential therapeutic applications.
Used in Drug Development:
Zacopride hydrochloride serves as a key component in the development of new drugs targeting the 5-HT3 receptor. Its antagonistic and agonistic properties make it a promising candidate for the creation of novel medications aimed at treating a range of conditions, including gastrointestinal disorders, anxiety, and other central nervous system-related issues.
Biological Activity
zacopride hydrochloride is a highly potent 5-ht3 receptor antagonist and 5-ht4 agonist (ki values are 0.38 and 373 nm, respectively) [1].5-ht3 and 5-ht4 receptors belong to 5-ht receptors which are a group of g protein-coupled receptor and ligand-gated ion channels located in the central and peripheral systems. 5-ht receptors play important roles in mediating both excitatory and inhibitory neurotransmission [1].on perifused human adrenocortical slices, administration of 20-min pulses of zacopride (10-11 ~ 10-6 mol/l) induced aldosterone secretion in a dose-dependent manner. the minimal effective dose was 10-10 mol/l, and half-maximal stimulation was achieved at a dose of 7 × 10-8 mol/l [2].in 28 healthy volunteers pretreated with dexamethasone, and then a single oral dose of placebo, 10 μg zacopride, or 400 μg zacopride, plasma aldosterone levels increased significantly within 90 min after the administration of 400 μg zacopride, remained elevated for 60 min, and gradually recovered to the baseline within 180 min. however, the administration of 10 μg zacopride or placebo did not modify the aldosterone concentration. no significant changes were observed in renin, adrenocorticotropic hormone, or cortisol levels [2].[1]. nagakura y, akuzawa s, miyata k, et al. pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-ht4 receptor versus human 5-ht3 receptor. pharmacological research, 1999, 39(5): 375-382.[2]. lefebvre h, contesse v, delarue c, et al. effect of the serotonin-4 receptor agonist zacopride on aldosterone secretion from the human adrenal cortex: in vivo and in vitro studies. the journal of clinical endocrinology and metabolism, 1993, 77(6): 1662-1666.
Biochem/physiol Actions
Zacopride is a sub-nanomolar antagonist of the serotonin 5-HT3 receptor that also displays agonist-like activity against 5-HT4 receptors. It is a potent anxiolytic in animal models, and also has strong antiemetic effects, and also increases aldosterone levels via activation of 5-HT4 receptor in the adrenal glands.
Check Digit Verification of cas no
The CAS Registry Mumber 101303-98-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,0,1,3,0 and 3 respectively; the second part has 2 digits, 9 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 101303-98:
(8*1)+(7*0)+(6*1)+(5*3)+(4*0)+(3*3)+(2*9)+(1*8)=64
64 % 10 = 4
So 101303-98-4 is a valid CAS Registry Number.
101303-98-4Relevant articles and documents
2-Alkoxy-n-(1-azabicyclo(2.2.2)-oct-3-yl) benzamides and thiobenzamides having an antischizophrenic activity
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, (2008/06/13)
2-Alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides having the formula wherein X is oxygen or sulphur; R1 is loweralkyl; and R2 is hydrogen, halo, 4,5-benzo, alkoxy or Am wherein Am is amino, methylamino or dimethylamino, and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof have antischizophrenic activity.
Method of using 2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide-N-oxides to control emesis caused by anticancer drugs
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, (2008/06/13)
A method of controlling emesis caused by anticancer drugs with 2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl) benzamide-N-oxides having the formula: STR1 wherein R1 is loweralkyl, and R2 is selected from the group consisting of hydrogen, halo, 4,5-benzo, methylsulfonyl, loweralkoxy or Am and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof is disclosed.
2-alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides
-
, (2008/06/13)
2-Alkoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamides and thiobenzamides having the formula STR1 wherein X is oxygen or sulfur; R1 is loweralkyl; and R2 is selected from the group consisting of hydrogen, halo, 4,5-benzo, alkoxy or Am and n is 1 or 2, and the pharmaceutically acceptable acid addition salts thereof having gastrokinetic and anti-emetic activity are disclosed.
