Functional and binding data for guinea-pig muscarinic receptor

• List of ligands
• List of receptors

Ligand	pA2 value	pD2 value	pPt value		Method	Comment
3-[2-(trifluoromethyl)phenoxyl]-1- azabicyclo[2.2.2.]octane ethanedioate (R)	6.83				1-01001	MODERATE COMPETITIVE ANTAGONISM.
3-[2-(trifluoromethyl)phenoxyl]-1- azabicyclo[2.2.2.]octane ethanedioate (R)		6.8			1-01001	MODERATE COMPETITIVE ANTAGONISM.
3-(4-hexyloxy-1,2,5-thiadiazol-3-yl) -1,2,5,6-tetrahydro-1-methylpyridine(Z)-2-butenedioate (1:1) salt		6.4			1-01001	3-(4-hexyloxy-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyridine(Z)-2-butenedioate (1:1) salt showed spasmogenic and tachyfylaxic activity at 1E-7M.
3-[4-(hexylthio)-1,2,5-thiadiazol-3-yl) -1,2,5,6-tetrahydro-1-methylpyridine(Z)-2-butenedioate		6.4			1-01001	3-[4-(hexylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyridine(Z)-2-butenedioate showed spasmogenic and tachyphylaxic activity.
4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl) benzonitrile monohydrochloride	4.3				1-01001	A VERY WEAK COMPETITIVE ANTAGONISM.
4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl) benzonitrile monohydrochloride	4.4				1-01001	VERY WEAK COMPETITIVE ANTAGONISM.
4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl) benzonitrile monohydrochloride		6.99			1-01001	VERY WEAK COMPETITIVE ANTAGONISM.
4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl) benzonitrile monohydrochloride		7			1-01001	A VERY WEAK COMPETITIVE ANTAGONISM.
4-[[[(3-chlorophenyl)amino]carbonyl]oxy]-N,N,N-trimethyl -2-butyn-1-aminiumchloride		6.7			1-01001	VERY VERY WEAK AGONISTIC ACTIVITY.
4-[[[(3-chlorophenyl)amino]carbonyl]oxy]-N,N,N-trimethyl -2-butyn-1-aminiumchloride		6.85			1-01001	NO ANTAGONISTIC ACTIVITY FOUND AT 3.0E-05 M. THE COMPOUND SHOWED WEAK SPASMOGENIC EFFECTS AT 3.0E-05 M.
4-[[[(3-chlorophenyl)amino]carbonyl]oxy]-N,N,N-trimethyl -2-butyn-1-aminiumchloride		<4			1-01001	VERY VERY WEAK AGONISTIC ACTIVITY.
4-[[[(3-chlorophenyl)amino]carbonyl]oxy]-N,N,N-trimethyl -2-butyn-1-aminiumchloride	<4.5				1-01001	NO ANTAGONISTIC ACTIVITY FOUND AT 3.0E-05 M. THE COMPOUND SHOWED WEAK SPASMOGENIC EFFECTS AT 3.0E-05 M.
4-damp bromide	8.7				1-01001	AGONIST STRONG COMPETITIVE AND RATHER STRONG NON- COMPETITIVE ANTAGONISM.
4-damp bromide	8.99				1-01001	pA2 SCHILD PLOT CALCULATED STRONG COMPETITIVE ANTAGONISM.
4-damp bromide		5.66			1-01001	AGONIST STRONG COMPETITIVE AND RATHER STRONG NON- COMPETITIVE ANTAGONISM.
4-damp bromide		6.91			1-01001	pA2 SCHILD PLOT CALCULATED STRONG COMPETITIVE ANTAGONISM.
4-damp bromide		7.8			1-01001	AGONIST STRONG COMPETITIVE AND RATHER STRONG NON- COMPETITIVE ANTAGONISM.
8-OH DPAT	5.4				1-01001	pA2 SCHILD-PLOT CALCULATED WEAK COMPETITIVE ANTAGONISM.
8-OH DPAT		7.1			1-01001	pA2 SCHILD-PLOT CALCULATED WEAK COMPETITIVE ANTAGONISM.
AF-102b/fks-508	4.9				1-01001	VERY WEAK COMPETITIVE ANTAGONISM AND AT HIGH CONCENTRATIONS A WEAK SPASMOGENIC EFFECT.
AF-102b/fks-508		5.3			1-01001	WEAK AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPIN SULFATE 1.0E-08 M.
AF-102b/fks-508		7.09			1-01001	VERY WEAK COMPETITIVE ANTAGONISM AND AT HIGH CONCENTRATIONS A WEAK SPASMOGENIC EFFECT.
AF-102b/fks-508		7.2			1-01001	WEAK AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPIN SULFATE 1.0E-08 M.
AF-30		4.9			1-01001	VERY WEAK AGONISTIC ACTIVITY, WHICH CAN BE BLOCKED BY ATROPINE 1.0E-8 M.
AF-30		7			1-01001	VERY WEAK AGONISTIC ACTIVITY, WHICH CAN BE BLOCKED BY ATROPINE 1.0E-8 M.
AF-DX 116 bs	6.18				1-01001
AF-DX 116 bs	6.1				1-01001	A MODERATE COMPETITIVE ANTAGONISM.
AF-DX 116 bs		5.74			1-01001
AF-DX 116 bs		6.98			1-01001	A MODERATE COMPETITIVE ANTAGONISM.
AH 6405		5.1			1-01001	SHOWED WEAK AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M.
AH 6405		6.6			1-01001	SHOWED WEAK AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M.
AHR 602		4			1-01001	VERY VERY WEAK AGONISTIC ACTIVITY.
AHR 602		6.7			1-01001	VERY VERY WEAK AGONISTIC ACTIVITY.
BHT 933		<4			1-01001	NO AGONISTIC ACTIVITY FOUND AT 1.0E-04 M.
RS 86 HBr		6.7			1-01001	A MODERATE AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M.
RS 86 HBr		6			1-01001	A MODERATE AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M.
UH-AH 37 HCl H2O	7.7				1-01001	Rather strong competitive antagonism.
UH-AH 37 HCl H2O		6.9			1-01001	Rather strong competitive antagonism.
YM796		5.2			1-01001	No antagonistic activity found at 3.0e-05 M. The compound showed weak agonistic activity, 50 times less potent than acetylcholine, which can be blocked by atropine sulfate 1.0e-08 M.
YM796		6.9			1-01001	No antagonistic activity found at 3.0e-05 M. The compound showed weak agonistic activity, 50 times less potent than acetylcholine, which can be blocked by atropine sulfate 1.0e-08 M.
YM796	<4.5				1-01001	No antagonistic activity found at 3.0e-05 M. The compound showed weak agonistic activity, 50 times less potent than acetylcholine, which can be blocked by atropine sulfate 1.0e-08 M.
aceclidine HCl		6.1			1-01001	MODERATE AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPIN
aceclidine HCl		7.01			1-01001	MODERATE AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPIN
arecaidine propargyl ester HCl		6.9			1-01001	RATHER STRONG AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M. BELL-SHAPED CRC'S.
arecaidine propargyl ester HCl		7.3			1-01001	RATHER STRONG AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M. BELL-SHAPED CRC'S.
arecoline HBr		6.5			1-01001	A MODERATE AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M.
arecoline HBr		6.8			1-01001	A MODERATE AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M.
bromerguride		5.9			1-01001	A WEAK NON-COMPETITIVE ANTAGONISM.
bromerguride		6.92			1-01001	A WEAK NON-COMPETITIVE ANTAGONISM.
buspirone HCl	4.4				1-01001	SHOWED VERY WEAK COMPETITIVE ANTAGONISM.
buspirone HCl		6.8			1-01001	SHOWED VERY WEAK COMPETITIVE ANTAGONISM.
cericlamine HCl	5.02				1-01001	WEAK COMPETITIVE AND VERY VERY WEAK NON- COMPETITIVE ANTAGONISM.
cericlamine HCl		3.7			1-01001	WEAK COMPETITIVE AND VERY VERY WEAK NON- COMPETITIVE ANTAGONISM.
cericlamine HCl		6.79			1-01001	WEAK COMPETITIVE AND VERY VERY WEAK NON- COMPETITIVE ANTAGONISM.
diaminopyridine (3,4-)		6.3			1-01001	SHOWED NO AGONISTIC ACTIVITY AT 1.0E-03 M.
diaminopyridine (3,4-)		<3			1-01001	SHOWED NO AGONISTIC ACTIVITY AT 1.0E-03 M.
dicyclomine HCl	7.84				1-01001	RATHER STRONG COMPETITIVE ANTAGONISM.
dicyclomine HCl		7.27			1-01001	RATHER STRONG COMPETITIVE ANTAGONISM.
ethylcholine iodide (o-)		6.5			1-01001	SHOWED MODERATE AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M.
ethylcholine iodide (o-)		6			1-01001	SHOWED MODERATE AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATROPINE SULFATE 1.0E-08 M.
flunarizine di-HCl		7.09			1-01001	A RATHER STRONG NON-COMPETITIVE ANTAGONISM.
flunarizine di-HCl		7.2			1-01001	A RATHER STRONG NON-COMPETITIVE ANTAGONISM.
fluperlapine	7.28				1-01001	RATHER STRONG COMPETITIVE ANTAGONISM.
fluperlapine		6.95			1-01001	RATHER STRONG COMPETITIVE ANTAGONISM.
idazoxan	4.5				1-01001	A VERY WEAK COMPETITIVE ANTAGONISM.
idazoxan		7.13			1-01001	A VERY WEAK COMPETITIVE ANTAGONISM.
isoarecoline HCl		5			1-01001	SHOWED A WEAK AGONISTIC ACTIVITY WHICH COULD BE BLOCKED BY A
isoarecoline HCl		7			1-01001	SHOWED A WEAK AGONISTIC ACTIVITY WHICH COULD BE BLOCKED BY A
ketanserin tartrate		3.9			1-01001	VERY VERY WEAK NON-COMPETITIVE ANTAGONISM.
ketanserin tartrate		7.19			1-01001	VERY VERY WEAK NON-COMPETITIVE ANTAGONISM.
mianserin HCl (racemate)	5.72				1-01001	WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM. AT HIGH CONC. A SPASMOGENIC EFFECT.
mianserin HCl (racemate)	5.74				1-01001	pA2 SCHILD-PLOT CALCULATED. 30 MIN. EQUIL. TIME WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM. AT HIGH CONC. A SPASMOGENIC EFFECT.
mianserin HCl (racemate)		4.5			1-01001	WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM. AT HIGH CONC. A SPASMOGENIC EFFECT.
mianserin HCl (racemate)		4.6			1-01001	pA2 SCHILD-PLOT CALCULATED. 30 MIN. EQUIL. TIME WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM. AT HIGH CONC. A SPASMOGENIC EFFECT.
mianserin HCl (racemate)		6.89			1-01001	pA2 SCHILD-PLOT CALCULATED. 30 MIN. EQUIL. TIME WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM. AT HIGH CONC. A SPASMOGENIC EFFECT.
mianserin HCl (racemate)		6.91			1-01001	WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM. AT HIGH CONC. A SPASMOGENIC EFFECT.
mianserin HCl R(-)	6.2				1-01001
mianserin HCl R(-)		7.05			1-01001
mianserin HCl S(+)	4.33				1-01001
mianserin HCl S(+)		4.2			1-01001
mianserin HCl S(+)		6.96			1-01001
minaprine 2HCl		7.12			1-01001	NO ANTAGONISTIC ACTIVITY FOUND AT 3.0E-05 M.
minaprine 2HCl	<4.5				1-01001	NO ANTAGONISTIC ACTIVITY FOUND AT 3.0E-05 M.
mirtazapine HCl (racemate)	6.13				1-01001
mirtazapine HCl (racemate)	6.13				1-01001
mirtazapine HCl (racemate)		6.84			1-01001
mirtazapine HCl (racemate)		6.84			1-01001
mirtazapine HCl R(-)	6.64				1-01001
mirtazapine HCl R(-)		7.21			1-01001
mirtazapine HCl S(+)	4.3				1-01001
mirtazapine HCl S(+)		6.93			1-01001
octanediamine (1,8-) diHCl		4			1-01001	84013: VERY WEAK ANTAGONISM.
octanediamine (1,8-) diHCl		7			1-01001	84013: VERY WEAK ANTAGONISM.
olanzapine	6.8				1-01001
olanzapine		7			1-01001
oxotremorine m		6.6			1-01001	RATHER STRONG AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATR
oxotremorine m		7.1			1-01001	RATHER STRONG AGONISTIC ACTIVITY WHICH CAN BE BLOCKED BY ATR
paroxetine HCl	5.6				1-01001
paroxetine HCl		5.1			1-01001
paroxetine HCl		6.7			1-01001
pindolol	4.4				1-01001	VERY WEAK COMPETITIVE ANTAGONISM.
pindolol		6.94			1-01001	VERY WEAK COMPETITIVE ANTAGONISM.
prazosin HCl	4.47				1-01001	A VERY WEAK COMPETITIVE ANTAGONISM.
prazosin HCl		6.9			1-01001	A VERY WEAK COMPETITIVE ANTAGONISM.
procyclidine HCl	7.86				1-01001	RATHER STRONG COMPETITIVE ANTAGONISM.
procyclidine HCl		6.93			1-01001	RATHER STRONG COMPETITIVE ANTAGONISM.
quinuclidinyl benzilate	8.95				1-01001	STRONG COMPETITIVE ANTAGONISM AND THE MAX. EFFECT FOR ACETYLCHOLINE WAS INCREASED.
quinuclidinyl benzilate		7.03			1-01001	STRONG COMPETITIVE ANTAGONISM AND THE MAX. EFFECT FOR ACETYLCHOLINE WAS INCREASED.
quinuclidinyl benzilate			8.7		1-01001	STRONG COMPETITIVE ANTAGONISM AND THE MAX. EFFECT FOR ACETYLCHOLINE WAS INCREASED.
rauwolscine HCl		4.1			1-01001	VERY WEAK NON-COMPETITIVE ANTAGONISM.
rauwolscine HCl		6.69			1-01001	VERY WEAK NON-COMPETITIVE ANTAGONISM.
risperidone	4.67				1-01001	VERY WEAK COMPETITIVE ANTAGONISM.
risperidone		6.73			1-01001	VERY WEAK COMPETITIVE ANTAGONISM.
ritanserin		6.08			1-01001	MODERATE NON-COMPETITIVE ANTAGONISM.
ritanserin		6.59			1-01001	MODERATE NON-COMPETITIVE ANTAGONISM.
ritanserin	<6				1-01001	MODERATE NON-COMPETITIVE ANTAGONISM.
secoverine HCl	7.72				1-01001	pA2 SCHILD PLOT CALCULATED RATHER STRONG COMPETITIVE ANTAGONISM.
secoverine HCl		6.89			1-01001	pA2 SCHILD PLOT CALCULATED RATHER STRONG COMPETITIVE ANTAGONISM.
telenzepine diHCl	7.89				1-01001	pA2 SCHILD PLOT CALCULATED RATHER STRONG COMPETITIVE ANTAGONISM.
telenzepine diHCl		6.93			1-01001	pA2 SCHILD PLOT CALCULATED RATHER STRONG COMPETITIVE ANTAGONISM.
vuf 8325		6.88			1-01001	NO ANTAGONISTIC ACTIVITY FOUND AT 3.0E-05 M.
vuf 8325	<4.5				1-01001	NO ANTAGONISTIC ACTIVITY FOUND AT 3.0E-05 M.
y-8894	5.37				1-01001	WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM.
y-8894		4.3			1-01001	WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM.
y-8894		7.08			1-01001	WEAK COMPETITIVE- AND VERY WEAK NON-COMPETITIVE ANTAGONISM.