R 715 TFA

R 715, a bradykinin B1 receptor antagonist, inhibits contractions in isolated human umbilical cords that express bradykinin B1 receptors (pA2 = 8.49) . When administered at doses of 200, 400, and 600 μg/kg, R 715 enhances latency to tail withdrawal in the tail-flick test for diabetic neuropathy mouse models induced by streptozotocin (STZ), signaling potential analgesic properties. Furthermore, at a 1 mg/kg per day dosage, it mitigates symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE) induced by MOG35-55 antigen peptide, such as reducing hind limb weakness and paralysis, improving gait symmetry, and decreasing spinal inflammation, neuron demyelination, and lesion monocyte invasion. Additionally, R 715 at 0.01 nmol/animal, administered intracerebroventricularly (i.c.v.), lowers mean arterial blood pressure and increases heart rate in spontaneously hypertensive rats, indicating cardiovascular effects.

O=C(N1[C@@H](CCC1)C(NCC(N[C@H](C(N[C@@H](CO)C(N[C@@H](C(N[C@H](C(O)=O)[C@@H](C)CC)=O)CC2=CC3=C(C=CC=C3)C=C2)=O)=O)CC4=CC=CC=C4)=O)=O)[C@H]5N(CCC5)C([C@H](CCCNC(N)=N)NC([C@@H](NC(C)=O)CCCCN)=O)=O.OC(C(F)(F)F)=O