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Gerhard Hallermayer

Boehringer Ingelheim

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Publication

Featured researches published by Gerhard Hallermayer.

British Journal of Pharmacology | 2000

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

Henri Doods; Gerhard Hallermayer; Dongmei Wu; Michael Entzeroth; Klaus Rudolf; Wolfhard Engel; Wolfgang Eberlein

Calcitonin gene‐related peptide (CGRP) is one of the most potent endogenous vasodilators known. This peptide is increased during migraine attacks and has been implicated in the pathogenesis of migraine headache. Here we report on the first small molecule selective CGRP antagonist: BIBN4096BS. In vitro, this compound is extremely potent at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM. In an in vivo model, BIBN4096BS in doses between 1 and 30 μg kg−1 (i.v.) inhibited the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. It is concluded that BIBN4096BS is a potent and selective CGRP antagonist.

Archive | 1997

Modified aminoacids, pharmaceuticals containing these compounds and method for their production

Klaus Rudolf; Wolfgang Eberlein; Wolfhard Engel; Helmut Pieper; Henri Doods; Gerhard Hallermayer; Michael Entzeroth; Wolfgang Wienen

Journal of Medicinal Chemistry | 2005

Development of Human Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists. 1. Potent and Selective Small Molecule CGRP Antagonists. 1-[N2-[3,5-Dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1- piperidinyl]carbonyl]-d-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: The First CGRP Antagonist for Clinical Trials in Acute Migraine†

Klaus Rudolf; Wolfgang Eberlein; Wolfhard Engel; Helmut Pieper; Michael Entzeroth; Gerhard Hallermayer; Henri Doods

European Journal of Pharmacology | 2000

Characterisation of calcitonin gene-related peptide receptors in rat atrium and vas deferens: evidence for a [Cys(Et)2,7]hCGRP-preferring receptor

Dongmei Wu; Wolfgang Eberlein; Klaus Rudolf; Wolfhard Engel; Gerhard Hallermayer; Henri Doods

Archive | 2004

Modified amino acids, pharmaceuticals containing these compounds and method for their production

Klaus Rudolf; Wolfgang Eberlein; Wolfhard Engel; Helmut Pieper; Henri Doods; Gerhard Hallermayer; Michael Entzeroth; Wolfgang Wienen

Archive | 2000

Antagonists of calcitonin gene-related peptide

Wolfgang Eberlein; Klaus Rudolf; Wolfhard Engel; Henri Doods; Gerhard Hallermayer

Archive | 2000

Arylalkane, arylalkene and aryl azaalkane, medicaments containing said compounds and method for the production thereof

Klaus Rudolf; Wolfgang Eberlein; Wolfhard Engel; Henri Doods; Gerhard Hallermayer; Eckhart Bauer

Archive | 2000

Modified amino-acid amides as cgrp antagonists

Wolfgang Eberlein; Klaus Rudolf; Wolfhard Engel; Henri Doods; Gerhard Hallermayer

Archive | 2007

Arylalkanes, arylalkenes and aryl-azaalkanes, pharmaceutical compositions containing these compounds and processes for preparing them

Klaus Rudolf; Wolfgang Eberlein; Wolfhard Engel; Henri Doods; Gerhard Hallermayer; Eckhart Bauer

Archive | 2005

Cyclopropane CGRP antagonists, medicaments containing these compounds, and method for the production thereof

Wolfgang Eberlein; Wolfhard Engel; Klaus Rudolf; Henri Doods; Gerhard Hallermayer; Eckhart Bauer

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Henri Doods

Boehringer Ingelheim

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Klaus Rudolf

Boehringer Ingelheim

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Wolfgang Eberlein

Boehringer Ingelheim

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Wolfhard Engel

Boehringer Ingelheim

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Michael Mark

Boehringer Ingelheim

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Ralph-Michael Budzinski

Boehringer Ingelheim

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Bernhard Eisele

Boehringer Ingelheim

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Roland Maier

Boehringer Ingelheim

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Michael Entzeroth

Boehringer Ingelheim

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Peter Müller

Boehringer Ingelheim

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