130497-33-5 Usage
Description
BRL 52537 HYDROCHLORIDE is a selective κ/μ ligand, known for its potent κ agonist properties. It has demonstrated the ability to attenuate ischemia-evoked nitric oxide production and serves as an effective analgesic agent.
Uses
Used in Pharmaceutical Industry:
BRL 52537 HYDROCHLORIDE is used as a potent analgesic agent for its ability to provide pain relief. It is particularly useful in managing various types of pain due to its κ agonist properties.
Used in Research and Development:
BRL 52537 HYDROCHLORIDE is used as a selective κ/μ ligand in research for its potential applications in understanding the mechanisms of pain and developing new therapeutic strategies for pain management.
Used in Cardiovascular Applications:
BRL 52537 HYDROCHLORIDE is used as a therapeutic agent for attenuating ischemia-evoked nitric oxide production, which can help in the treatment and management of cardiovascular conditions related to ischemia.
Biological Activity
The most κ / μ -selective and among the most potent κ ligands known (25 times more potent than morphine in vivo ).
Check Digit Verification of cas no
The CAS Registry Mumber 130497-33-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,0,4,9 and 7 respectively; the second part has 2 digits, 3 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 130497-33:
(8*1)+(7*3)+(6*0)+(5*4)+(4*9)+(3*7)+(2*3)+(1*3)=115
115 % 10 = 5
So 130497-33-5 is a valid CAS Registry Number.
InChI:InChI=1/C18H24Cl2N2O.ClH/c19-16-7-6-14(11-17(16)20)12-18(23)22-10-2-1-5-15(22)13-21-8-3-4-9-21;/h6-7,11,15H,1-5,8-10,12-13H2;1H
130497-33-5Relevant articles and documents
New κ-Receptor Agonists Based upon a 2-piperidine Nucleus
Scopes, David I. C.,Hayes, Norman F.,Bays, David E.,Belton, David,Brain, John,et al.
, p. 490 - 501 (2007/10/02)
The syntheses of some 1--2-piperidines and their activities as κ-opioid receptor agonists are described.Selected structural modifications are made to the basic moiety and at the 2-, 3-, 4-, 5-, and 6-positions on the piperidine nucleus to enable structure-activity relationships to be delineated.As a result, some highly potent and selective κ-receptor agonists have been identified.In particular, this has been achieved by introduction of oxygen-containing functionality into the 4-position of the piperidine nucleus or the 3-position of the pyrrolidinylmethyl side chain.Thus, 1--2-piperidine (10) possesses high activity in the rabbit vas deferens (LVD, κ-specific tissue) (IC50 = 0.20 nM) and is a potent antinociceptive agent, as determined by the mouse acetylcholine-induced abdominal constriction test (MAC) (ED50 = 0.06 mg/kg, sc).The spirocyclic analogue 8--7-(1-pyrrolidinylmethyl)-1,4-dioxa-8-azaspirodecane (39) showed exceptionally potent activity: LVD, IC50 = 0.10 nM; MAC, ED50 = 0.001 mg/kg, sc.Both 10 and 39 displayed high selectivity for κ-opioid receptors over both μ- and δ-opioid receptor subtypes.
