High affinity relaxin receptors, polypeptide compositions related thereto,
as well as nucleotide compositions encoding the same, are provided. These
proteins, herein termed LGR7 and LGR8, are orphan
leucine-repeat-containing, G protein-coupled receptors. These receptors
have a wide and a unique tissue expression pattern. The receptors,
particularly soluble fragments thereof, are useful as therapeutic agents
capable of inhibiting the action of relaxin and InsL3. The receptors and
fragments thereof also find use in the screening and design of relaxin
agonists and antagonists. Conditions treatable with relaxin agonists or
antagonists include prevention or induction of labor, treatment of
endometriosis, treatment of skin conditions such as scleroderma that
require collagen or extracellular matrix remodelling. Additionally,
relaxin has been implicated in the dilation of blood vessels' smooth
muscle cells directly and through release of nitric oxide and atrial
natriuretic peptide. Relaxin has also been used in the treatment of
severe chronic pain, particularly pain arising from stretching, swelling,
or dislocation of tissues.