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HomeProduct name listOPC 21268

OPC 21268

Synonym(s):1-{1-[4(3-acetylaminopropoxy)benzoyl]-4-piperidyl}-3,4-dihydro-2(1H)-quinolinone hydrate;N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide hydrate

OPC 21268 Structural

What is OPC 21268?

Description

OPC 21268 is a nonpeptide antagonist of vasopressin V1 receptors (IC50 = 0.4 μM in rat liver membranes). It is selective for V1 over V2 receptors (IC50 = >100 μM in kidney membranes). It is also selective for rat over human V1 receptors (Kis = 25 and 8,800 nM, respectively), which can be partially attributed to the alanine residue at position 337 of the rat sequence, instead of a glycine residue in the human sequence, with differences at positions 224, 310, and 324 also contributing. OPC 21268 (0.03-1 mg/kg, i.v.) inhibits pressor responses induced by arginine vasopressin (argipressin; ) in pithed rats and arginine vasopressin-induced vasoconstriction in conscious rats (ID50 = 2 mg/kg). It induces hypotension in aged spontaneously hypertensive rats (SHRs) and stroke-prone SHRs when administered at a dose of 3 mg/kg.

The Uses of OPC 21268

OPC 21268 is a nonpeptide AVP (Vasopressin) Receptor V antagonist.

What are the applications of Application

OPC 21268 is a nonpeptide AVP (Vasopressin) Receptor V antagonist

Storage

Store at +4°C

Properties of OPC 21268

Boiling point: 772.5±60.0 °C(Predicted)
Density  1?+-.0.06 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMSO: ≥20mg/mL
pka 16.17±0.46(Predicted)
form  powder
color  white to off-white

Safety information for OPC 21268

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
ghs
Environment
GHS09
GHS Hazard Statements H302:Acute toxicity,oral
H400:Hazardous to the aquatic environment, acute hazard
Precautionary Statement Codes P273:Avoid release to the environment.

Computed Descriptors for OPC 21268

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