Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist

British Journal of Pharmacology

Volumn 129, Issue 3, 2000, Pages 420-423

  Doods, Henri ^a   Hallermayer, Gerhard ^a   Wu, Dongmei ^a   Entzeroth, Michael ^a   Rudolf, Klaus ^a   Engel, Wolfhard ^a   Eberlein, Wolfgang ^a  

^a BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

Author keywords

BIBN4096BS; CGRP antagonist; Migraine

Indexed keywords

CALCITONIN GENE RELATED PEPTIDE; CALCITONIN GENE RELATED PEPTIDE RECEPTOR; OLCEGEPANT; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BLOOD FLOW; CONTROLLED STUDY; DRUG POTENCY; FEMALE; HUMAN; HUMAN CELL; MALE; MARMOSET; MIGRAINE; NERVE STIMULATION; NONHUMAN; PRIMATE; PRIORITY JOURNAL; RAT; TRIGEMINUS GANGLION; VASODILATATION;

EID: 0033970471     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703110     Document Type: Article

References (17)

1. Aiyar, N., Rand, K., Elshourbagy, N.A., Zeng, Z., Adamou, J.E., Bergsma, D.J. & Li, Y. (1996). A cDNA encoding the calcitonin gene-related peptide type 1 receptor. J. Biol. Chem., 271, 11325-11329.
2. Amara, S.G., Jones, V., Rosenfeld, M.G., Ong, E.S. & Evans, R.M. (1982). Alternative RNA processing in calcitonin gene expression generates mRNA encoding different polypeptide products. Nature, 298, 240-244.
3. Brain, S.D. & Cambridge, H. (1996). Calcitonin Gene-Related Peptide: Vasoactive Effects and Potential Therapeutic Role. Gen. Pharmacol., 27, 607-611.
4. 50) of an enzymatic reaction. Biochem. Pharmacol., 22, 3099-3105.
5. Chiba, T., Yamaguchi, A., Yamatani, T., Nakamura, A., Morishita, T., Inui, T., Fukase, M., Noda, T. & Fujita, T. (1989). Calcitonin gene-related peptide receptor antagonist human CGRP(8-37). Am. J. Physiol., 256, E331-E335.
6. Escott, K.J., Beattie, D.T., Connor, H.E. & Brain, S.D. (1995). Trigeminal ganglion stimulation increases facial skin blood flow in the rat: a major role for calcitonin gene-related peptide. Brain Research, 669, 93-99.
7. Gallai, V., Sarchielli, P., Floridi, A., Franceschini, M., Codini, M., Glioti, G., Trequattrini, A. & Palumbo, R. (1995). Vasoactive peptide levels in the plasma of young migraine patients with and without aura assessed both interictally and ictally. Cephalalgia, 15, 384-390.
8. Goadsby, P.J., Edvinsson, L. & Ekman, R. (1988). Release of vasoactive peptides in the extracerebral circulation of humans and the cat during activation of the trigeminovascular system. Ann. Neurol., 23, 193-196.
9. Goadsby, P.J., Edvinsson, L. & Ekman, R. (1990). Vasoactive peptide release in the extracerebral circulation of humans during migraine headache. Ann. Neurol., 28, 183-187.
10. Goadsby, P.J. & Edvinsson, L. (1993). The trigemino-vascular system and migraine: studies characterizing cerebrovascular and neuropeptide changes seen in humans and cats. Ann. Neurol., 33, 48-56.
11. Goadsby, P.J., Zagami, A.S. & Lambert, G.A. (1991). Neural processing of craniovascular pain: a synthesis of the central structures involved in migraine. Headache, 31, 365-371.
12. Moskowitz, M.A. (1984). The neurobiology of vascular head pain. Ann Neurol., 16, 157-168.
13. Moskowitz, M.A. & MacFarlane, R. (1993). Neurovascular and molecular mechanisms in migraine headaches. Cerebrovasc. Brain Metab. Rev., 5, 159-177.
14. Rist, B., Entzeroth, M. & Beck-Sickinger, A.G. (1998). From micromolar to nanomolar affinity: a systematic approach to identify the binding site of CGRP at the human calcitonin gene-related peptide 1 receptor. J. Med. Chem., 41, 117-123.
15. Rudolf, K., Eberlein, W., Engel, W., Beck-Sickinger, A.G., Wittneben, H., Wieland, H.A. & Doods, H.N. (1997). BIBP3226, a potent and selective neuropeptide Y Y1-receptor antagonist. Structure-activity studies and localization of the human Y1 receptor binding site. In: Grundemar, L. & Bloom, S.R. (eds). Neuropeptide Y and drug development, pp. 175-190.
16. x and competitive drug antagonism. Brit. J. Pharmacol., 4, 277-280.
17. Sexton, P.M. (1991). Central nervous binding sites for calcitonin and calcitonin gene-related peptide. Mol. Neurobiol., 5, 251-273.