title: Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat.
abstract: The design and synthesis of two closely related series of prostacyclin receptor agonist compounds that showed excellent human IP receptor potency and efficacy is described. Compounds from this series showed in vivo activity after SC dosing in the monocrotaline model of PAH in rat.
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Thuy-Anh
authors: TA
authors: Tran
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Young-Jun
authors: YJ
authors: Shin
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Bryan
authors: B
authors: Kramer
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Juyi
authors: J
authors: Choi
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Ning
authors: N
authors: Zou
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Pureza
authors: P
authors: Vallar
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Peter
authors: P
authors: Martens
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: P Douglas
authors: PD
authors: Boatman
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: John W
authors: JW
authors: Adams
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Juan
authors: J
authors: Ramirez
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Yunqing
authors: Y
authors: Shi
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Michael
authors: M
authors: Morgan
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: David J
authors: DJ
authors: Unett
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Steve
authors: S
authors: Chang
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Hsin-Hui
authors: HH
authors: Shu
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA.
authors: Shiu-Feng
authors: SF
authors: Tung
authors: Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA. Electronic address: gsemple@arenapharm.com.
authors: Graeme
authors: G
authors: Semple
mesh_terms: D000818:Animals; D055808:Drug Discovery; D006801:Humans; D006976:Hypertension, Pulmonary / Q000139:chemically induced / Q000188:drug therapy*; D016686:Monocrotaline; D010974:Platelet Aggregation / Q000187:drug effects; D051381:Rats; D011982:Receptors, Prostaglandin / Q000819:agonists* / Q000378:metabolism
chemical_list: D011982:Receptors, Prostaglandin; D016686:Monocrotaline
keywords: GPCR; IP receptor agonist; PAH; Prostacyclin