Results 301 to 310 of about 205,233 (331)
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Specific GABAA agonists and partial agonists
The Chemical Record, 2002AbstractThe GABAA receptor system is implicated in a number of neurological and psychiatric diseases, making GABAA receptor ligands interesting as potential therapeutic agents. Only a few different classes of structures are currently known as ligands for the GABA recognition site on the hetero‐pentameric GABAA receptor complex, reflecting the very ...
Krogsgaard-Larsen, Povl +2 more
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Partial agonists and acetylcholine liberation
European Journal of Pharmacology, 1970Abstract The effects of cooling, tetrodotoxin, cocaine, atropine, dibenamine and of a mixture of tetrodotoxin, cocaine and hexamethonium on the actions of cholinesters, alkyltrimethylammonium salts and dimethylaminoethanol derivatives were tested on the guinea pig small intestine.
K, Takagi, I, Takayanagi, F, Taga
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Partial Agonist Activity of Celiprolol
Journal of Cardiovascular Pharmacology, 1993Celiprolol given intravenously (i.v.) to pithed rats in the dose range of 0.1-10,000 micrograms/g produced a dose-dependent increase in heart rate (HR) which was greatest (123 beats/min) at 1,000-3,000 micrograms/kg. This partial agonist effect was blocked by the selective beta 1-adrenoceptor antagonist CGP 20712A.
L H, Tung +5 more
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Agonists, partial agonists, antagonists, inverse agonists and agonist/antagonists?
Trends in Pharmacological Sciences, 1987The label placed on a drug influences its ultimate use. But interpretation ofin-vivo data has complicated the simple receptor theory of agonists and antagonists for certain classes of drugs.Terry Kenakin argues that clarification of such data — described in an extremely complex system — at a molecular level, will either obviate the need for terms such ...
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Synthetic glucagon antagonists and partial agonists
International Journal of Peptide and Protein Research, 1991This 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.
C, Zechel, D, Trivedi, V J, Hruby
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Novel antioestrogens without partial agonist activity
Journal of Steroid Biochemistry, 1988The oestrogenic and antioestrogenic properties of some novel 7 alpha-alkyl amide derivatives of 17 beta-oestradiol have been measured in rats and mice. The compound ICI 164384 was devoid of oestrogenic activity in the uterus and vagina of both species and on the hypothalamic-pituitary axis of the rat.
A E, Wakeling, J, Bowler
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Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines
Journal of Medicinal Chemistry, 1989The synthesis and biochemical evaluation of a series of oxadiazole derivatives of imidazobenzodiazepines related to the benzodiazepine antagonist Ro 15-1788 (2a) are reported. Although the oxadiazole ring is seen as an isosteric replacement for the ester linkage, significant differences in structure-activity trends were observed.
Frank Watjen +11 more
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Dopamine receptor partial agonists and addiction
European Journal of Pharmacology, 2015Many 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.
Fabricio A, Moreira, Jeffrey W, Dalley
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Partial dopamine agonists in schizophrenia
British Journal of Hospital Medicine, 2005The 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 ...
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Pharmacotherapy for tobacco cessation: Nicotine agonists, antagonists, and partial agonists
Current Oncology Reports, 2007Nicotine replacement therapies (NRT) were the main pharmacologic option for treatment of nicotine dependence until the early 1990s, when controlled clinical trials confirmed the efficacy of bupropion, the first treatment not based on nicotine. Varenicline, a partial agonist at nicotine receptors, gained US regulatory approval in 2006 for smoking ...
Maher, Karam-Hage, Paul M, Cinciripini
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