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Bioorg Med Chem Lett. 1998 Aug 18;8(16):2111-6.

3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.

Abstract

Pyridyloxypropanolamines L-749,372 (8, beta 3 EC50 = 3.6 nM) and L-750,355 (29, beta 3 EC50 = 13 nM) are selective partial agonists of the human receptor, with 33% and 49% activation, respectively. Both stimulate lipolysis in rhesus monkeys (ED50 = 2 and 0.8 mg/kg, respectively), with minimal effects on heart rate. Oral bioavailability in dogs, 41% for L-749,372 and 47% for L-750,355, is improved relative to phenol analogs.

PMID:
9873496
DOI:
10.1016/s0960-894x(98)00381-3
[Indexed for MEDLINE]

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