Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo [3.1. 0] hexane-2, 6-dicarboxylic acid (LY354740): a potent, selective, and orally active …

…, JP Tizzano, MJ Kallman, DR Helton… - Journal of medicinal …, 1997 - ACS Publications
2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (9) was designed as a conformationally
constrained analog of glutamic acid. For 9, the key torsion angles (τ 1 and τ 2 ) which …

Anxiolytic and side-effect profile of LY354740: a potent, highly selective, orally active agonist for group II metabotropic glutamate receptors

DR Helton, JP Tizzano, JA Monn, DD Schoepp… - … of Pharmacology and …, 1998 - ASPET
LY354740 is a conformationally constrained analog of glutamate which is a potent agonist
for group II cAMP coupled metabotropic glutamate receptors (mGluRs). The discovery of this …

2-Substituted (2SR)-2-Amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as Potent and Selective Antagonists of Group II Metabotropic Glutamate Receptors. 2 …

…, BG Johnson, JP Tizzano, DR Helton… - Journal of medicinal …, 1998 - ACS Publications
In this paper we describe the synthesis of a series of α-substituted analogues of the potent
and selective group II metabotropic glutamate receptor (mGluR) agonist (1S,1‘S,2‘S)-…

Nicotine withdrawal: a behavioral assessment using schedule controlled responding, locomotor activity, and sensorimotor reactivity

DR Helton, DL Modlin, JP Tizzano, K Rasmussen - Psychopharmacology, 1993 - Springer
Three different behavioral measures were used to assess the effects of abrupt cessation of
chronic nicotine treatment. Nicotine (0, 3, or 6 mg/kg per day) was continuously administered …

Urotensin II acts as a modulator of mesopontine cholinergic neurons

…, CJ Tyler, DM Duangdao, SL Grupke, DR Helton… - Brain research, 2005 - Elsevier
Urotensin II (UII) is a vasomodulatory peptide that was not predicted to elicit CNS activity.
However, because we have recently shown that the urotensin II receptor (UII-R) is selectively …

Serotonin‐1A antagonists attenuate the effects of nicotine withdrawal on the auditory startle response

K Rasmussen, MJ Kallman, DR Helton - Synapse, 1997 - Wiley Online Library
Withdrawal from the chronic administration of nicotine has previously been shown to lead to
an enhanced auditory startle response in rats. In order to explore the neuropharmacology …

The proconvulsive activity of quinolone antibiotics in an animal model

PD Williams, DR Helton - Toxicology letters, 1991 - Elsevier
The side-effect profile of quinolone antibiotics in man includes CNS disturbances such as
dizziness, insomnia and convulsions. Although it has been suggested that the proconvulsive …

Central nervous system characterization of the new cholecystokininB antagonist LY288513

DR Helton, JE Berger, JF Czachura… - Pharmacology …, 1996 - Elsevier
The activity of LY288513, an investigational cholecystokinin (CCK) B antagonist, was evaluated
in a wide range of pharmacological tests in mice and rats. The anxiolytic benzodiazepine…

Pharmacokinetic profiles in rats after intravenous, oral, or dermal administration of dapsone

DR Helton, DW Osborne, SK Pierson… - Drug metabolism and …, 2000 - ASPET
Dapsone is a potent anti-inflammatory and antibacterial agent that has been used extensively
in the oral treatment of leprosy and dermatitis herpetiformis. This study compared the …

Intracerebral 1S, 3R-1-aminocyclopentane-1, 3-dicarboxylic acid (1S, 3R-ACPD) produces limbic seizures that are not blocked by ionotropic glutamate receptor …

JP Tizzano, KI Griffey, JA Johnson, AS Fix, DR Helton… - Neuroscience …, 1993 - Elsevier
The functional role of metabotropic glutamate receptor (mGluR) activation was investigated
following intracerebral administration of 1S,3R-ACPD in mice. Injections of 1S,3R-ACPD (50–…