extravasation

Zolmitriptan (311C90) selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries and 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brainstem sensory nuclei. Zolmitriptan is a member of the triptan class of agents with anti-migraine properties. Receptor binding results in constriction of cranial vessels, reduction of vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relieve migraine headaches by inhibition of pro-inflammatory neuropeptide release.

N-Acetylneuraminic acid (Acide aceneuramique) is a nine-carbon sialic acid monosaccharide commonly found in glycoproteins on cell membranes and in glycolipids such as gangliosides in mammalian cells. Studies have shown that N-Acetylneuraminic acid is biologically useful for neurotransmission, leukocyte extravasation, viral or bacterial infections, and carbohydrate-protein recognition.

BF-1 is a novel selective 5-HT2 receptor antagonist that acts by blocking neurogenic dural plasma protein extravasation induced by mCPP or BW723C86.BF-1 is used in the study of migraine.

5'-N-Ethylcarboxamidoadenosine (NECA), an agonist of the Adenosine receptor, increases cerebral extravasation of fluorescein and low molecular weight dextran independent of blood-brain barrier modulation.

Ac2-12 TFA, an annexin lipocortin 1 (LC1)-mimetic peptide, inhibits neutrophil extravasation and demonstrates antimigratory effects by attenuating the recruitment of neutrophils in experimental models of inflammation [1] [2].

Urotensin-II (UT) receptor ligand; behaves as a silent antagonist in most in vitro assays and in vivo, but does retain small residual agonist activity under certain conditions in some assays. Competitively antagonizes U-II induced contractions in the rat

GW833972 is a CB2 Agonist. GW 833972A inhibited capsaicin-induced depolarization of the human and guinea-pig and prostaglandin E(2) (PGE(2)) and hypertonic saline-induced depolarization of the guinea-pig isolated vagus nerve in vitro. GW 833972A also inhibited citric acid-induced cough but not plasma extravasation in the guinea-pig and this effect was blocked by a CB(2) receptor antagonist.

4991W93 is a 5HT(1B/1D) receptor partial agonist, inhibiting electrically induced plasma extravasation, blocking neurogenic plasma protein extravasation, inhibiting release of calcitonin gene-related peptide.

Enlimomab (BI-RR 0001), a murine IgG2a monoclonal antibody targeting human ICAM-1, reduces leukocyte adhesion to the vascular endothelium, diminishing leukocyte extravasation and inflammatory tissue damage; it exhibits anti-inflammatory properties and is utilized in stroke research [1] [2].

CP-122288 is a potent and selective agonist for the 5-HT1B, 5-HT1D and 5-HT1F serotonin receptor subtypes. CP-122288 is potent as an inhibitor of plasma protein extravasation and neurogenic inflammation.

PNU109291, a potent and selective agonist of the 5-HT1D receptor, effectively mitigates dural plasma extravasation induced by trigeminal ganglion stimulation.

Annexin/lipocortin 1-mimetic peptide; inhibits leukocyte extravasation. Reduces neutrophil adhesion and emigration, and promotes detachment of neutrophils from activated mesenteric endothelium in mice in vivo.

N-terminal peptide of Annexin I (AI/Lipocortin I) that inhibits leukocyte extravasation. Acts as a formyl peptide receptor 1 (FPR1) ligand and stimulates neutrophil NADPH oxidase activation.