Allan K. Uldam
ACADIA Pharmaceuticals Inc.
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Publication
Featured researches published by Allan K. Uldam.
Journal of Pharmacology and Experimental Therapeutics | 2006
Kimberly E. Vanover; David M. Weiner; Malath Makhay; Isaac Veinbergs; Luis R. Gardell; Jelveh Lameh; Andria L. Del Tredici; Fabrice Piu; Hans H. Schiffer; Thomas R. Ott; Ethan S. Burstein; Allan K. Uldam; Mikkel Boas Thygesen; Nathalie Schlienger; Carl Magnus Andersson; Thomas Son; Scott C. Harvey; Susan B. Powell; Mark A. Geyer; Bo-Ragner Tolf; Mark R. Brann; Robert E. Davis
The in vitro and in vivo pharmacological properties of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103) are presented. A potent 5-hydroxytryptamine (5-HT)2A receptor inverse agonist ACP-103 competitively antagonized the binding of [3H]ketanserin to heterologously expressed human 5-HT2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. ACP-103 displayed potent inverse agonist activity in the cell-based functional assay receptor selection and amplification technology (R-SAT), with a mean pIC50 of 8.7. ACP-103 demonstrated lesser affinity (mean pKi of 8.80 in membranes and 8.00 in whole cells, as determined by radioligand binding) and potency as an inverse agonist (mean pIC50 7.1 in R-SAT) at human 5-HT2C receptors, and lacked affinity and functional activity at 5-HT2B receptors, dopamine D2 receptors, and other human monoaminergic receptors. Behaviorally, ACP-103 attenuated head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (1-10 mg/kg s.c.) induced by the 5-HT2A receptor agonist (±)-2,5-dimethoxy-4-iodoamphetamine hydrochloride in rats and reduced the hyperactivity induced in mice by the N-methyl-d-aspartate receptor noncompetitive antagonist 5H-dibenzo[a,d]cyclohepten-5,10-imine (dizocilpine maleate; MK-801) (0.1 and 0.3 mg/kg s.c.; 3 mg/kg p.o.), consistent with a 5-HT2A receptor mechanism of action in vivo and antipsychotic-like efficacy. ACP-103 demonstrated >42.6% oral bioavailability in rats. Thus, ACP-103 is a potent, efficacious, orally active 5-HT2A receptor inverse agonist with a behavioral pharmacological profile consistent with utility as an antipsychotic agent.
Life Sciences | 2001
Daniel W. Gil; Tracy A. Spalding; Alex Kharlamb; Niels Skjaerbaek; Allan K. Uldam; Carol Trotter; Donghui Li; Elizabeth Woldemussie; Larry A. Wheeler; Mark R. Brann
Pilocarpine has been used to lower intraocular pressure (IOP) in glaucoma patients for more than 100 years. Since the identification of five muscarinic receptor subtypes, there has been an interest in separating the IOP-lowering effects from the ocular side effects of pupil constriction and lens accommodation. However, all these actions seem to be mediated by the M3 receptor. A novel muscarinic receptor agonist, AGN 199170, that has no activity on the M3 subtype was compared to pilocarpine in a monkey glaucoma model. This compound lowered IOP suggesting that muscarinic agonists targeted at muscarinic receptors other than the M3 subtype may be able to selectively lower IOP.
Archive | 2004
David M. Weiner; Robert E. Davis; Mark R. Brann; Carl-Magnus A. Andersson; Allan K. Uldam
Archive | 2001
Carl-Magnus A. Andersson; Glenn Croston; Eva-Louise Hansen; Allan K. Uldam
Archive | 2011
Carl-Magnus A. Andersson; Glenn Croston; Eva Louise Hansen; Allan K. Uldam
Archive | 2004
David M. Weiner; Robert E. Davis; Mark R. Brann; Norman Nash; Carl-Magnus A. Andersson; Allan K. Uldam
Archive | 2004
David M. Weiner; Robert E. Davis; Mark R. Brann; Norman Nash; Carl Magnus Andersson; Allan K. Uldam
Archive | 2004
Carl-Magnus A. Andersson; Mark R. Brann; Robert E. Davis; Norman Nash; Allan K. Uldam; M.David Weiner
Archive | 2004
M.David Weiner; Robert E. Davis; Mark R. Brann; Norman Nash; Carl-Magnus A. Andersson; Allan K. Uldam
Archive | 2004
Robert E. Davis; David M. Weiner; Mark R. Brann; Norman Nash; Carl-Magnus A. Andersson; Allan K. Uldam