M-cholinoblocking activity of IMPERIALINE and its derivatives compared with that of ATROPINE.

	ION CHANNEL and RECEPTOR LIGANDS TOXINS & ALKALOIDS M-cholinoblocking activity of IMPERIALINE and its derivatives compared with that of ATROPINE.

M-cholinoblocking activity of IMPERIALINE and its derivatives compared with that of ATROPINE

CODE	SUBSTANCE NAME	ACTIVITY LEVEL (%) ON FOLLOWING ORGANS			RELATIVE ACTIVITY LEVEL M2:M4:M3	DURATION OF THE EFFECT
		HEART (M2)	INTESTINE (M4)	SALIVARY GLANDS (M3)
	ATROPINE	100	100	100	1:1:1	Medium
L6008	IMPERIALINE	25	1.2	0.1	250:12:1	Short
L6050	IMPERIALONE	78	4.8	0.27	290:17:1	Medium
L6033	3-b-Chloro-IMPERIALINE	180	13	0.3	600:40:1	Medium
L6032	3-a-Chloro-IMPERIALINE	290	70	8	36:9:1	Long
L6099	3-b-Bromo-IMPERIALINE	65	1.7	0.16	406:10:1	Medium
The above figures show that 3-a-Chloro-Imperialine presents the highest M-cholinoblocking activities. However, its selectivity between M₂ and M₄ is the lowest. 3-b-Chloro-Imperialine combines a high M₂-blocking activity with good selectivity levels. 3-b-Bromo-Imperialine is the most M₂/M₄ selective and may also be a precursor of the labelled Imperialine derivative 3-a-¹²⁵I-Imperialine.

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