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SER-100 is a peripherally acting, highly potent and selective partial agonist of the nociceptin/orphanin FQ peptide (NOP) receptor, also known as the opioid receptor-like 1 (ORL1) receptor. It was developed by coupling a chain of six lysine residues to an existing NOP receptor partial agonist hexapeptide (Ac-RYYRWK-NH2), which improved its metabolic stability. The drug is classified as an oligopeptide/peptide and has been investigated primarily for cardiovascular indications such as isolated systolic hypertension and pulmonary hypertension. In clinical studies, subcutaneous administration of SER-100 in patients with isolated systolic hypertension resulted in significant reductions in both systolic and diastolic blood pressure compared to placebo, with an acceptable safety profile. Its mechanism involves modulation of vascular tone via peripheral NOP receptors, leading to hypotensive and bradycardic effects[1][3][5][6].
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