1052147-86-0 Usage
Uses
Used in Pharmaceutical Research:
LP-211 is used as a research compound for studying the serotonin 5-HT7 receptor's role in various physiological and pathological processes. Its agonistic activity on the receptor makes it a valuable tool for understanding the receptor's function and potential therapeutic applications.
Used in Antidepressant Development:
As a selective agonist for the serotonin 5-HT7 receptor, LP-211 is used in the development of novel antidepressant drugs. The serotonin 5-HT7 receptor has been implicated in mood regulation, and targeting this receptor may provide a new approach to treating depression and related disorders.
Used in Brain Penetration Studies:
LP-211 is a brain penetrant compound, making it useful for studying the transport of drugs across the blood-brain barrier. This property is crucial for developing medications that can effectively treat central nervous system (CNS) disorders, such as neurodegenerative diseases and psychiatric conditions.
Used in Metabolic Studies:
Pharmacological studies have shown that LP-211 undergoes metabolic breakdown to RA-7, which also exhibits pharmacological activities. This makes LP-211 a valuable compound for studying metabolic pathways and the potential effects of its metabolites on various physiological processes.
Used in Temperature Regulation Research:
LP-211 has been shown to induce hypothermia in mice, making it a useful compound for studying the mechanisms underlying temperature regulation and the potential development of drugs that can modulate body temperature for therapeutic purposes.
Used in Pharmacokinetic Studies:
LP-211 has demonstrated optimal pharmacokinetics in rats, making it a valuable compound for studying the absorption, distribution, metabolism, and excretion of drugs. Understanding these pharmacokinetic properties is essential for the development of safe and effective medications.
Biochem/physiol Actions
LP-211 is a brain penetrant selective agonist for the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor. The 5-HT7 receptor is involved in a variety of central nervous system functions including circadian rhythm, sleep, thermoregulation, nociception, and memory, and appears to be involved in cognitive disorders, anxiety, and depression. LP-211 has been used as a selective 5-HT7 receptor agonist in multiple models including studies as a potential therapeutic agent in models of Rett syndrome and Fragile X Syndrome.
Check Digit Verification of cas no
The CAS Registry Mumber 1052147-86-0 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,5,2,1,4 and 7 respectively; the second part has 2 digits, 8 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1052147-86:
(9*1)+(8*0)+(7*5)+(6*2)+(5*1)+(4*4)+(3*7)+(2*8)+(1*6)=120
120 % 10 = 0
So 1052147-86-0 is a valid CAS Registry Number.
1052147-86-0Relevant articles and documents
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1- piperazinehexanamides: Influence on lipophilicity and 5-HT7 receptor activity. Part III
Leopoldo, Marcello,Lacivita, Enza,De Giorgio, Paola,Fracasso, Claudia,Guzzetti, Sara,Caccia, Silvio,Contino, Marialessandra,Colabufo, Nicola A.,Berardi, Francesco,Perrone, Roberto
experimental part, p. 5813 - 5822 (2009/09/08)
Starting from the previously reported 5-HT7 receptor agents 4-7 with N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamide structure, the 1-(2-methylthiophenyl)-, 1-(2-diphenyl)-, 1(2-isopropylphenyl)-, and 1-(2-methoxyphenyl)pipe
