SB-706375 is a potent, surmountable, reversible and selective mammalian urotensin-II receptor antagonist. In rats SB-706375 provoked a pronounced diuresis and natriuresis, accompanied by modest increases in effective renal blood flow and glomerular filtration rate.

N-Methylspiperone (NMSP) is a derivate of spiperone and high-affinity D2/3 dopamine and 5-HT2A serotonin receptor antagonist. In the biodistribution studies in rodents, there was a high accumulation of radioactivity in the liver, lung, and kidneys, whereas the brain radioactivity was not as high N-Methylspiperone is used to study the dopamine and serotonin neurotransmitter systems. Labeled with the radioisotope carbon-11, it can be used for positron emission tomography (PET). [11C] N-Methylspiperone PET is useful for objective monitoring of D2and 5-HT2A receptor occupancy and density in patients being treated with antipsychotic drugs.

HMR 1031 is a potent and specific antagonist of the integrin VLA-4 (alpha4beta1) binding to vascular cell adhesion molecule-1 (VCAM-1) and fibronectin. HMR 1031 is an inhaled drug being developed for the treatment of asthma using an Ultrahaler dry-powder inhalation device. The interaction of VLA-4 with VCAM-1 is involved in the extravasations, activation, and extravascular survival of mononuclear leukocyte and eosinophil cell types at sites of airway inflammation. Thus, the VLA-4 antagonist, HMR 1031, has potential as an anti-inflammatory agent.

CP 99994 dihydrochloride have shown the compound to be a potent, selective and competitive NK-1 receptor antagonist. In preclinical studies, CP 99994 decreased cough number, peak abdominal activity, and peak tracheal pressure, without affecting baseline respiration. But in clinical trial administration of CP 99994 over 2 h does not significantly inhibit hypertonic saline-induced bronchoconstriction or cough in subjects with mild asthma. CP 99994 significantly suppressed acute postoperative pain at 90 min after surgery.

MDL 201012 is a muscarinic M3 receptor antagonist.