Anatibant

Product NameAnatibant
CAS209733-45-9
MFC34H36Cl2N6O5S
MW711.66
EINECS
MOL File209733-45-9.mol

Chemical Properties

Density	1.44±0.1 g/cm3(Predicted)
pka	14.09±0.46(Predicted)

Usage And Synthesis

Uses

Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases[1][2].

Definition

ChEBI: Anatibant is a proline derivative.

in vivo

Anatibant (3 mg/kg; subcutaneous bolus; injection 15 min and 8 h after trauma, respectively) significantly reduces intracranial pressure (ICP) and of contusion volume 24 h after trauma in treated mice^[1].

Animal Model:	Male C57/Bl6 mice (25-28 g) were subjected to Controlled Cortical Impact trauma (CCI)^[1]
Dosage:	3 mg/kg
Administration:	Subcutaneous bolus; injection 15 min and 8 h after trauma, respectively
Result:	Demonstrated a significant reduction of ICP and of contusion volume 24 h after trauma in treated mice.

IC 50

Bradykinin B2 Receptor (B2R): 0.67 nM (Ki, human recombinant B2 receptor); Bradykinin B2 Receptor (B2R): 1.74 nM (Ki, Rat recombinant B2 receptor); Bradykinin B2 Receptor (B2R): 1.37 nM (Ki, Guinea-pig recombinant B2 receptor)

References

[1] Klaus Zweckberger, et al. Anatibant, a selective non-peptide bradykinin B2 receptor antagonist, reduces intracranial hypertension and histopathological damage after experimental traumatic brain injury. Neurosci Lett. 2009 Apr 24;454(2):115-7. DOI:10.1016/j.neulet.2009.02.014
[2] D Pruneau, et al. Pharmacological profile of LF 16-0687, a new potent non-peptide bradykinin B2 receptor antagonist. Immunopharmacology. 1999 Sep;43(2-3):187-94. DOI:10.1016/s0162-3109(99)00128-9

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