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Anti‐peptide antibodies sensitive to the ‘active’ state of the β 2 ‐adrenergic receptor
Author(s) -
Mijares Alfredo,
Lebesgue Diane,
Argibay Jorge,
Hoebeke Johan
Publication year - 1996
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(96)01321-x
Subject(s) - agonist , inverse agonist , receptor , alprenolol , peptide , chemistry , antibody , alpha 1a adrenergic receptor , alpha 1d adrenergic receptor , antagonist , partial agonist , adrenergic , microbiology and biotechnology , endocrinology , beta 1 adrenergic receptor , biology , biochemistry , beta 3 adrenergic receptor , immunology
Antibodies directed against a peptide corresponding to the second loop of the human β 2 ‐adrenergic receptor were induced in rabbits by immunisation with the free peptide in complete Freund's adjuvant. The resulting antibodies were affinity‐purified and shown to be monospecific for the target receptor. They were able to stimulate the L‐type Ca 2+ channels in whole‐cell patch‐clamp experiments on isolated adult guineapig cardiomyocytes. This effect was similar to that obtained by the specific β 2 ‐adrenergic agonist zinterol. The antibody effects could be blocked with the specific β 2 ‐adrenergic inverse agonist ICI118,551 but not with the neutral antagonist alprenolol. These results suggest that the antibodies recognise the active conformer of the β 2 ‐adrenergic receptor.