Results 311 to 320 of about 195,829 (332)

GABAA Receptor Agonists, Partial Agonists, and Antagonists

1997
The neutral amino acid, γ-aminobutyric acid (GABA), is an inhibitory transmitter in the central nervous system (CNS). Furthermore, GABA is involved as a neurotransmitter and/or a paracrine effector in the regulation of a variety of physiological mechanisms in the periphery.
Frølund, Bente, Krogsgaard-Larsen, Povl, Ebert, Bjarke   +2 more
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Identification of a PPARδ agonist with partial agonistic activity on PPARγ

Bioorganic & Medicinal Chemistry Letters, 2009
The discovery and optimization of a series of potent PPARdelta full agonists with partial agonistic activity against PPARgamma is described.
Richard V. Connors, Yang Li, Sheree Johnstone, Nigel Walker, Athena Sudom, Anne Chai, Peter Coward, Brian M. Fox, Malgorzata Wanska, Alex Zhang, Karen Siegler, Zhulun Wang, Steve Hiscock, Martin Harrison, Michael Dore, Jinsong Liu, Marc Labelle   +16 more
openaire   +3 more sources

Dopamine receptor agonists, partial agonists and psychostimulant addiction

Trends in Pharmacological Sciences, 1994
Despite the epidemic growth of psychostimulant addiction over the past years, few pharmacological means of intervention are available to date for clinical treatment. This is of importance since the withdrawal syndrome that follows abstinence from drugs such as cocaine and the amphetamines is characterized, among other symptoms, by intense craving for ...
Luigi Pulvirenti, George F. Koob
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Partial dopamine agonists in schizophrenia

British Journal of Hospital Medicine, 2005
The emergence of partial dopamine agonists reinforces the argument for the dopamine hypothesis of schizophrenia. Aripiprazole (Abilify®) is the first of these compounds for the treatment of schizophrenia to be launched in the UK. Aripiprazole has a promising efficacy and favourable tolerability profile that suggests it has a significant role to play ...
openaire   +3 more sources

Oxyfedrine — A partial agonist at β-adrenoceptors

European Journal of Pharmacology, 1972
Abstract Oxyfedrine, 0.5 μg/ml, caused typical but long lasting sympathomimetic effects on guinea-pig atria and trachealis, rabbit atria and duodenum and rat uterus and perfused heart. These effects were antagonised by propranolol. The heart rate and blood pressure of the anaesthetised rat also showed sympathomimetic responses.
R.W. Foster, P.R. Beckett
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Cardiopulmonary Effects of Narcotic Agonists and a Partial Agonist in Horses

American Journal of Veterinary Research, 1978
SUMMARY The cardiopulmonary effects of the narcotic agonists morphine, meperidine, oxymorphone, and methadone and of the partial agonist pentazocine were examined in the pain-free adult horse. The drugs produced dysphoric followed by euphoric effects. Increases in heart rate, arterial blood pressure, and cardiac output were observed in all horses with ...
W W, Muir, R T, Skarda, W C, Sheehan
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Synthetic glucagon antagonists and partial agonists

International Journal of Peptide and Protein Research, 1991
This paper reports the synthesis and the biological activities of six new glucagon analogues. In these compounds N‐terminal modifications of the glucagon sequence were made, in most cases combined with changes in the C‐terminal region which had been shown previously to enhance receptor affinity.
Dev Trivedi, Christian Zechel, Victor J. Hruby   +2 more
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Dopamine receptor partial agonists and addiction

European Journal of Pharmacology, 2015
Many drugs abused by humans acutely facilitate, either directly or indirectly, dopamine neurotransmission in the mesolimbic pathway. As a consequence dopamine receptor agonists and antagonists have been widely investigated as putative pharmacological therapies for addiction.
Jeffrey W. Dalley, Fabricio A. Moreira, Fabricio A. Moreira   +2 more
openaire   +3 more sources

Measurement of partial agonist activity of pindolol

Clinical Pharmacology and Therapeutics, 1981
The partial agonist activity of pindolol was assessed by examining the action of cumulative doses on the heart rate of resting, standing, and exercising healthy men and by studying the interaction of pindolol with metoprolol, a beta blocker devoid of partial agonist activity.
S. George Carruthers, Yaw Twum-Barima
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Antiestrogens and Partial Agonists

1999
For more than a decade, the antiestrogen tamoxifen dominated the field of estrogen antagonists despite its inherent estrogenicity. For a long time, efforts to replace tamoxifen or improve its pharmacological profile by structural modifications have failed.
openaire   +2 more sources