A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine. Migraine.

MK-0974(Telcagepant) is a highly potent, selective, and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively; displays >1500-fold lower affinity for the canine and rat receptors

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.

Olcegepant hydrochloride is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.

Olcegepant(BIBN 4096; BIBN 4096BS) is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor(IC50= 0.03 nM).

Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.

PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism.

Adrenomedullin (16-31), human TFA is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human TFA possesses pressor activity in the systemic vascular bed of the rat, but not the cat.

Calcitonin human is an endogenous calcitonin receptor agonist.Calcitonin human lowers systemic blood calcium levels and inhibits bone resorption.

Vazegepant (BHV-3500) hydrochloride is a highly soluble CGRP receptor antagonist. Vazegepant hydrochloride is the first intranasal gepant for migraine. Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation.

Vazegepant is the first intranasal CGRP receptor antagonist for the study the acute research of migraine.

HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute treatment of migraine.

SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis.

BMS-846372 (BMS846372) is a potent, selective, orally active CGRP receptor antagonist with Ki of 0.07 nM (hCGRP).BMS-846372 inhibited CGRP-stimulated cAMP production in SK-N-MC cells with IC50 of 0.22 nM, could completely inhibited CGRP-mediated elevation of cAMP.BMS-846372 showed exposure-dependent inhibition of CGRP-induced increases in marmoset facial blood flow upon subcutaneous (sc) dosing in hαCGRP-induced increases in facial blood flow model.

FE 205030 (FE205030) is a potent, selective peptidic CGRP antagonist with IC50 of 0.2 nM.FE 205030 displays>100,000 fold against hAM1R and >6363 fold against hAM2R tested in Human CGRP, AM1R and AM2R receptor cAMP assays.FE 205030 inhibited CGRP-induced vasodilation in isolated human mesenteric resistance arteries in an ex vivo isometric myograph study; effectively blocked CGRP-induced vasodilation with a pA2 of 9.3.FE 205030 is a first in class injectable fast acting selective and potent agent for the treatment of acute episodic migraine.

(3R,5R,6S)-Atogepant ((3R,5R,6S)-MK-8031) is the enantiomer of Atogepant. Atogepant is a calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.

BMS-694153 is a potent, selective calcitonin gene-related peptide (CGRP) receptor antagonist with Ki of 0.013 nM for hCGRP (inhibition of 125I-CGRP binding in SK-N-MC cell membranes).