Agonists nicotinic

CH H L C—0—C—C—N—CH II 1 H, 1 0 CH CH Metacholine - -h++ + Muscarine, however, is not the major poison of toadstool that spot is taken by muscimol, which has antimuscarinergic effect Treatment 

Cholinergic antagonists have a larger therapeutie role than agonists. Again, we can distinguish drugs that selectively affect nicotinic and muscarinic receptors. 

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Grady, S.R., Meinerz, N.M., Cao, J. et al. Nicotinic agonists stimulate acetylcholine release from mouse interpeduncular nucleus a function mediated by a different nAChR than dopamine release from striatum. J. Neurochem. 76 258, 2001. 

Lendvai, B., Sershen, H., Lajtha, A. et al. Differential mechanisms involved in the effect of nicotinic agonists DMPP and lobeline to release [3H]5-HT from rat hippocampal slices. Neuropharmacology. 35 1769, 1996. 

Figure 18.2 Structures of progenitor nicotinic agonists and hERG activities.

Linville DG, Williams S, Raszkiewicz JL, Arneric SP. (1993). Nicotinic agonists modulate basal forebrain control of cortical cerebral blood flow in anesthetized rats. J Pharmacol Exp Ther. 267(1) 440-48. 

Nanri M, Kasahara N, Yamamoto J, Miyake H, Watanabe H. (1998). A comparative study on the effects of nicotine and GTS-21, a new nicotinic agonist, on the locomotor activity and brain monoamine level. Jpn J Pharmacol. 78(3) 385-89. 

Stoierman IP, Garcha HS, Mirza NR. (1995). Dissociations between the iocomotor stimulant and depressant effects of nicotinic agonists in rats. Psychopharmacology (Berlin). 117(4) 430-37. 

Damaj MI, Creasy KR, Welch SP, Rosecrans JA, Aceto MD, Martin BR. (1995). Comparative pharmacology of nicotine and ABT-418, a new nicotinic agonist. Psychopharmacoiogy (Berlin). 

It is well established that nicotine, and other nicotinic agonists, will elicit Ca++-dependent release of dopamine from striatal tissue slices (see, for examples... 

Badio B, Daly JW (1994) Epibatidine, a potent analgetic and nicotinic agonist. Mol Pharmacol 45 563-569... 

Sharpies CG, Kaiser S, SoUakov L, Marks MJ, Collins AC, Washburn M, Wright E, Spencer JA, Gallagher T, Whiteaker P, Wonnacott S (2000) UB-165 a novel nicotinic agonist with subtype selectivity implicates the alpha4beta2 subtype in the modulation of dopamine release from rat striatal synaptosomes. J Neurosci 20 2783-2791... 

Drug discrimination is also an imporfanf sfandard technique used in assessments of the abuse liability of novel psychoactive compounds, with relevance to attempts to develop novel nicotinic agonists for use as cognitive enhancers. 

In conclusion, studies with nicotinic agonists are compatible with the view that oc4p2-containing receptors play a critical and possibly unique role in generating the discriminative stimulus properties of nicotine. 

Chance WT, Murfin D, Krynock GM, Rosecrans lA (1977) A description of the nicotine stimulus and tests of its generahzation to amphetamine. Psychopharmacology 55 19-26 Chance WT, KaUman MD, Rosecrans lA, Spencer RM (1978) A comparison of nicotine and structurally related compounds as discriminative stimuli. Br 1 Pharmacol 63 609-616 Chandler Cl, Stolerman IP (1997) Discriminative stimulus properties of the nicotinic agonist cytisine. Psychopharmacology 129 257-264... 

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