Biomaterial Database

Inhibition of adenylate cyclase and stimulation of a high affinity GTPase by the antilipolytic agents, nicotinic acid, acipimox and various related compounds. 1983

K Aktories, and G Schultz, and K H Jakobs

In hamster adipocyte ghosts, the influence of the antilipolytic agents, nicotinic acid, 5-methyl-pyrazine-2-carboxylic acid 4-oxide (acipimox) and various related compounds, was studied on adenylate cyclase and low Km GTPase activities. As shown before for hormonal factors and nicotinic acid, the new drug, acipimox, inhibited adenylate cyclase by a GTP-dependent process, which was amplified by sodium ions; half-maximal inhibition occurred at about 10 mumol/l acipimox. For the various compounds studied, the following rank order of potency in inhibition of adenylate cyclase was obtained, nicotinic acid greater than 3-carboxy-5-methylpyrazole greater than acipimox greater than 3-carboxy-5-methylisoxazole; 6-hydroxynicotinic acid and beta-pyridylcarbinol had no effect up to 300 mumol/l. In the same membrane system the antilipolytic drugs increased GTP hydrolysis by stimulation of a low Km GTPase as shown before for antilipolytic hormones. The potency order of the antilipolytic agents studied was identical for GTPase stimulation and adenylate cyclase inhibition. The data suggest that the antilipolytic drugs studied act on adipocyte adenylate cyclase via membrane-bound receptors in a hormone-like manner and that stimulation of a high affinity GTPase is involved in the mechanism of adenylate cyclase inhibition by these agents.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D009525	Niacin	A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.	Nicotinic Acid,3-Pyridinecarboxylic Acid,Enduracin,Induracin,Lithium Nicotinate,Niacin Aluminum Salt,Niacin Ammonium Salt,Niacin Calcium Salt,Niacin Cobalt (2+) Salt,Niacin Copper (2+) Salt,Niacin Hydrochloride,Niacin Iron (2+) Salt,Niacin Lithium Salt,Niacin Lithium Salt, Hemihydrate,Niacin Magnesium Salt,Niacin Manganese (2+) Salt,Niacin Potassium Salt,Niacin Sodium Salt,Niacin Tartrate,Niacin Tosylate,Niacin Zinc Salt,Nicamin,Nico-400,Nicobid,Nicocap,Nicolar,Nicotinate,Wampocap,3 Pyridinecarboxylic Acid,Aluminum Salt, Niacin,Hydrochloride, Niacin,Nico 400,Nico400,Nicotinate, Lithium,Potassium Salt, Niacin,Sodium Salt, Niacin,Tartrate, Niacin,Tosylate, Niacin
D010744	Phosphoric Monoester Hydrolases	A group of hydrolases which catalyze the hydrolysis of monophosphoric esters with the production of one mole of orthophosphate.	Phosphatase,Phosphatases,Phosphohydrolase,Phosphohydrolases,Phosphomonoesterase,Phosphomonoesterases,Phosphoric Monoester Hydrolase,Hydrolase, Phosphoric Monoester,Hydrolases, Phosphoric Monoester,Monoester Hydrolase, Phosphoric
D011719	Pyrazines	A heterocyclic aromatic organic compound with the chemical formula C4H4N2.	Pyrazine
D004822	Epididymis	The convoluted cordlike structure attached to the posterior of the TESTIS. Epididymis consists of the head (caput), the body (corpus), and the tail (cauda). A network of ducts leaving the testis joins into a common epididymal tubule proper which provides the transport, storage, and maturation of SPERMATOZOA.
D006224	Cricetinae	A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.	Cricetus,Hamsters,Hamster
D000067956	Adenylyl Cyclase Inhibitors	Compounds that bind to and inhibit the action of ADENYLYL CYCLASES.	Adenylate Cyclase Inhibitors,Cyclase Inhibitors, Adenylate,Cyclase Inhibitors, Adenylyl,Inhibitors, Adenylate Cyclase,Inhibitors, Adenylyl Cyclase
D000273	Adipose Tissue	Specialized connective tissue composed of fat cells (ADIPOCYTES). It is the site of stored FATS, usually in the form of TRIGLYCERIDES. In mammals, there are two types of adipose tissue, the WHITE FAT and the BROWN FAT. Their relative distributions vary in different species with most adipose tissue being white.	Fatty Tissue,Body Fat,Fat Pad,Fat Pads,Pad, Fat,Pads, Fat,Tissue, Adipose,Tissue, Fatty
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D000960	Hypolipidemic Agents	Substances that lower the levels of certain LIPIDS in the BLOOD. They are used to treat HYPERLIPIDEMIAS.	Antihyperlipidemic,Antilipemic,Antilipemic Agents,Antilipemic Drug,Hypolipidemic Agent,Hypolipidemic Drug,Antihyperlipemics,Antihyperlipidemics,Antilipemic Drugs,Antilipemics,Hypolipidemic Drugs,Agent, Hypolipidemic,Agents, Antilipemic,Agents, Hypolipidemic,Drug, Antilipemic,Drug, Hypolipidemic,Drugs, Antilipemic,Drugs, Hypolipidemic