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Role of muscarinic receptors in cardiovascular regulation in SHR
Published in H. Saito, Y. Yamori, M. Minami, S.H. Parvez, New Advances in SHR Research –, 2020
As constantly new antagonists for muscarinic receptors are developed, the list given in Table 1 only represents a small but well investigated selection. Several compounds, for example, posses a high affinity for M1-receptors, the most widely used M1-antagonists being pirenzepine and telenzepine (Hammer et al., 1980). However, they also show an affinity for M3- and M2-receptors. M2-selective drugs, as for example AF-DX 116 or himbacine, still exhibit an intermediate affinity for M1-receptors (Giachetti et al., 1986) whereas compounds, that have a high affinity for the M3 receptor, generally also exhibit a high affinity for the M1-receptor (Doods et al., 1987).
Briefing Therapeutic Approaches in Anticoagulant, Thrombolytic, and Antiplatelet Therapy
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
Vorapaxar (Figure 7.15) is a thrombin receptor (protease-activated receptor, PAR-1) antagonist based on the natural product himbacine. It is given to patients with a history of myocardial infarction (heart attack) or persons with peripheral arterial disease [97].
Neurotransmission at Parasympathetic Nerve Endings
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Discrimination between M2 and M4 receptor-mediated responses may be achieved with AF-DX 116 which shows M2 selectivity compared with all other subtypes. Himbacine may separate M4 from M1 receptors, having higher affinity for M4(Lazareno et al. 1990). Recent studies suggest that himbacine can also distinguish different M1 subtypes in the rabbit vas deferens (pA2 = 8.17) and rat superior cervical ganglion (pA2 = 7.14) (Sagrada et al. 1993). The Ki value for displacement of binding in the hippocampus or cerebral cortex was 7.0. Muscarinic receptors in the hippocampus have been designated M1α while those of the ganglia may be M1β.
Alpha2‐adrenoceptor agonists inhibit form‐deprivation myopia in the chick
Published in Clinical and Experimental Optometry, 2019
Brittany J Carr, Cynthia T Nguyen, William K Stell
Off‐target binding of drugs is not a well‐studied line of inquiry, but there is interesting evidence from the chick form‐deprivation model that supports a role for off‐target, and not muscarinic, receptor effects for myopia treatment with high concentrations of atropine, himbacine, and MT3. Atropine and himbacine are very potent inhibitors of the chick mAChR M4 receptor (710-pmol/L and 6-nmol/L, respectively), yet a high concentration of these drugs is required to achieve full inhibition of form‐deprivation myopia in the chick.