Cholinergic receptors muscarinic

Nicotinic Receptor Agonists. There has been significant activity in the development of muscarinic cholinergic receptor agonists for dementia. In addition, agents that interact with nicotinic cholinergic receptors may also have therapeutic value. Nicotinic receptors have been reported to be... 

Ward, D., and Trevor, A. Phencyclidine-induced alteration in rat muscarinic cholinergic receptor regulation. ux U Pharmacol 74 189-193, 1981. 

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. 

Antihistamines are commonly used to prevent and treat nausea and vomiting due to motion sickness, vertigo, or migraine headache.1,17 Their efficacy is presumably due to the high concentration of histamine (Hx) and muscarinic cholinergic receptors within the vestibular system. Similarly to scopolamine, antihistamines such as diphenhydramine and... 

Monoamine oxidase inhibition Serotonin reuptake inhibition Norepinephrine reuptake inhibition Dopamine reuptake inhibition a2-Adrenergic receptor blockade Serotonin-2A receptor blockade Serotonin-2C receptor blockade Serotonin-3 receptor blockade op-Adrenergic receptor blockade Histamine-1 receptor blockade Muscarinic cholinergic receptor blockade... 

Gronier, B. Rasmussen, K. (1998). Activation of midbrain presumed dopaminergic neurones by muscarinic cholinergic receptors an in vivo electrophysiological study in the rat. Br. J. Pharmacol. 124, 455-64. 

ACh regulates the cortical arousal characteristic of both REM sleep and wakefulness (Semba, 1991, 2000 Sarter Bruno, 1997, 2000). Medial regions of the pontine reticular formation (Figs. 5.2 and 5.7) contribute to regulating both the state of REM sleep and the trait of EEG activation. Within the medial pontine reticular formation, presynaptic cholinergic terminals (Fig. 5.1) that release ACh also are endowed with muscarinic cholinergic receptors (Roth et al, 1996). Autoreceptors are defined as presynaptic receptors that bind the neurotransmitter that is released from the presynaptic terminal (Kalsner, 1990). Autoreceptors provide feedback modulation of transmitter release. Autoreceptor activation... 

EEG slow waves. The differential EEG and ACh responses to dialysis delivery of AF-DX 116 (M2/M4) versus pirenzepine (M1/M4) supports the conclusion that, in B6 mouse, postsynaptic muscarinic receptors of the Ml subtype form one receptor mechanism by which ACh activates the EEG (Douglas et al, 2002a). The data summarized in Fig. 5.11 provide direct measures of G protein activation in basal forebrain and prefrontal cortex by muscarinic cholinergic receptors (DeMarco et al, 2004). The in vitro data of Fig. 5.11A indicate the presence of functional muscarinic receptors in regions of B6 mouse prefrontal cortex where in vivo microdialysis studies (Douglas et al, 2002a, b) revealed modulation of ACh release and EEG by pre- and postsynaptic muscarinic receptors (Figs. 5.9 and 5.10). 

Scopolamine A muscarinic cholinergic receptor antagonist that has amnesic side effects. 

The pharmacotherapy of first choice for UUI is anticholinergic/antispas-modic drugs, which antagonize muscarinic cholinergic receptors. 

Eriksson and co-workers have reported that neonatal exposure to low doses of the pyrethroids bioallethrin and deltamethrin by oral administration from postnatal days 10 to 16 induced an increase in muscarinic cholinergic receptor (MAChR) density in cerebral cortex at the age of 17 days. That resulted in a decrease in the cortical MAChR density, an increase in motor activity, and a lack of habituation at the adult age of 4 months in mice [48-50]. 

Respiratory Effects. Information on respiratory effects due to exposure to disulfoton is very limited. Exposure to disulfoton causes overstimulation of the muscarinic cholinergic receptors in the respiratory tract (Murphy 1986). This usually results in excessive bronchial secretions, bronchoconstriction, and eventually respiratory failure. Pulmonary edema and hemoptysis were recognized as probable causes of death in a man who ingested an unknown amount of disulfoton (Hattori et al. 1982). Studies regarding inhalation exposure were concerned primarily with lethality or cholinesterase inhibition. However, in intermediate-duration inhalation studies in rats, inflammation... 

Jones, S.B. and King, L.B. 1995, Muscarinic cholinergic receptors in brain and atrial membranes of adult Brook Trout Salvelinus fontinalis measured by radiolignad binding techniques. Comp. Biochem. Physiol. 112 43-50. 

Steevens, J.A. Bauman, P.C. Jones, S.B. 1996, A comparison of (3-adrenoceptors and muscarinic cholinergic receptors in tissues of brown bullhead catfish Ameiurus nebulosus from die Black River and Old Woman Creek Ohio. Environ. Toxciol. Chem. 15 1551-1554. 

Cortes R, Palacios JM. (1986). Muscarinic cholinergic receptor subtypes in the rat brain. I. 

---