Cholinergic receptors, stimulation

Rosecrans JA, Chance WT (1978) The discriminative stimulus properties of n- and m-cholinergic receptor stimulants. In Ho BT, Richards DW III, Chute DL (eds) Drug discrimination and state dependent learning. Academic, New York, pp 119-130 Rosecrans JA, Schechter MD (1972) Brain area nicotine levels in male and female rats of two strains. Arch Int de Pharmacodynamic et de Therapie 196 46-54 Rosecrans JA, Kallman MJ, Glennon RA (1978) The nicotine cue an overview. In Colpaert EC, Rosecrans JA (eds) Stimulus properties of drugs ten years of progress. Elsevier-North Holland, Amsterdam, pp 69-81... 

Grando, S.A., Horton, R.M., Mauro, T.M., Kist, D.A., Lee, T.X., and Dahl, M.V., Activation of keratinocyte nicotinic cholinergic receptors stimulates calcium influx and enhances cell differentiation, /. Invest. Dermatol. 107, 412-418, 1996. 

Histamine receptors were first divided into two subclasses Hi and H2 by Ash and Schild (1966) on the basis that the then known antihistamines did not inhibit histamine-induced gastric acid secretion. The justification for this subdivision was established some years later when Black (see Black et al. 1972) developed drugs, like cimetidine, that affected only the histamine stimulation of gastric acid secretion and had such a dramatic impact on the treatment of peptic ulcers. A recently developed H2 antagonist zolantidine is the first, however, to show significant brain penetration. A further H3 receptor has now been established. It is predominantly an autoreceptor on histamine nerves but is also found on the terminals of aminergic, cholinergic and peptide neurons. All three receptors are G-protein-coupled but little is known of the intracellular pathway linked to the H3 receptor and unlike Hi and H2 receptors it still remains to be cloned. Activation of Hi receptors stimulates IP3 formation while the H2 receptor is linked to activation of adenylate cyclase. 

Motion sickness is caused by stimulation of the vestibular system. This area contains many histaminic (Hj) and muscarinic cholinergic receptors. The higher brain (i.e., cerebral cortex) is affected by sensory input such as sights, smells, or emotions that can lead to vomiting. This area is involved in anticipatory nausea and vomiting associated with chemotherapy. 

Reverses age-related decline in choline acetyltransferase Reverses an age-related decline in muscarinic receptors Stimulates learning-related cholinergic activity Monoamine Facilitates release of norepinephrine (through o2)... 

March M, Risso F, Viola C, Cavazzani P, Raiteri M (2002) Direct evidence that release-stimulating alpha7 nicotinic cholinergic receptors are localized on human and rat brain glutamatergic axon terminals. J Neurochem 80 1071-1078... 

Mecfianism of Action A cholinergic-receptor agonist that binds to acetylcholine receptors, producing both stimulating and depressant effects on the peripheral and central nervous systems. Therapeutic Effect Provides a source of nicotine during nicotine withdrawal and reduces withdrawal symptoms. 

The answer is d. (Hardman, pp 192-193.) Nicotine is a depolarizing ganglionic blocking agent that initially stimulates and then blocks nicotinic muscular (NM) (skeletal muscle) and nicotinic neural (NN) (parasympathetic ganglia) cholinergic receptors. Blockade of the sympathetic division of the autonomic nervous system (ANS) results in arteriolar vasodilation, bradycardia, and hypotension. Blockade at the neuromuscu-... 

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