High affinity ghrelin receptor agonist (pKi
= 8.14). Growth hormone (GH) secretagog; stimulates GH release from rat pituitary cells in vitro
= 1.3 nM) and enhances GH plasma levels in vivo
. Also attenuates isoproterenol
-induced lipolysis in rat adipocytes in vitro
. Orally bioavailable.
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All Tocris products are intended for laboratory research use only.
Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Galpha(o1) by the Ghrelin receptor.
Bennett et al.
Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue.
Patchett et al.
Ghrelin and des-acyl ghrelin both inhibit isoproterenol-induced lipolysis in rat adipocytes via a non-type 1a growth hormone secretagogue receptor.
Mucciolo et al.