Agonist for all muscarinic receptors (M₁, M₂, M₃) and for all nicotinic receptors (N_N, N_M)

This is an acetic acid ester and so it is susceptible to AChE.

This does not have B-methyl group so it is active at nicotinic receptors.

Quaternary amine with positive charge, poor lipid solubility, doesn't absorb well or get to CNS

Antagonist to all muscarinic receptors (M₁, M₂, M₃)

Terteriay amine, so it aborbs wel, can get into CNS

Not a target for AChE

Removed by kindeys

Agonist to all muscarinic rececptors (M₁, M₂, M₃)

This is a carbamic acid ester, so it is negligibly susceptible to AChE

The B-methyl group makes it less active at nicotinic receptors.

Quaternary amine with positive charge, poor lipid solubility, doesn't absorb well or get to CNS

Agonist for B₁, A₁ and A₂

(not particularly agonistic for B₂)

HEART! Nerves, smooth muscle

(Also some skeletal muscles have M₂ receptors that are activated by the sympathetic nervous system, leading to dilation of blood vessels there)

Glands, smooth muscle, epithelium (though there is no parasympathetic innervation to the M₃ receptors in the epithelial cells!)

(Sphincter muscle of the pupil, ciliary muscle of the eye, bronchiole smooth muscle, bronciole glands, detrusor muscle of the urinary bladder, salivary glands, smooth muscle of intestines, smooth muscle of the stomach)

Of note: The M₃ receptors in the internal sphincter of the urinary bladder leads to relaxation of the muscle there, instead of the usual contraction!)

Also, some skeletal muscle vessels might have M₃ receptors that respond to sympathetic innervation...

Smooth muscles of the vessels and prostate

(radial muscle of pupil, internal sphincter of the urinary bladder, smooth muscle of arteries and veins)

Presynaptic sites, smooth muscle, platelets, fat cells

(Presynaptic sites as modifiers of parasympathetic output (decrease it!))

Smooth and Cardiac muscles

(Atria, Ventricles, SA node, AV Node, Perkinje fibers, urinary bladder detrusor muscle)

(Also bronchiole smooth muscles, but there is not really sympathetic innervation here. They more respond to epinephrine put out by the adrenal medulla)

Remember B₂ doesn't realyl respond to norepinephrine.

Smooth muscle, brown adipose tissue

(Detrusor muscle of the urinary bladder)

Smooth muscle contraction (G_q protein leads to more DAG and IP3, which make more calcium available for contraction)

Exception: Internal Sphincter of the Urinary Bladder

Beta receptors are coupled with the G_s protien, which makes for more cAMP and more PKA. More PKA leads to more phosphorlation of calcium channels to let more calcium into the cells, and more phosphorlation of phospholambin which increases calcium uptake into the sarcoplasmic reticulum.

(Important to remember that cardiac muscle, unlike smooth muscle, has a calcium input from the outside. More calcium coming in!)

M₂ receptors use G_i protiens. This means there is less cAMP, less PKA and thus less inward calcium current.

Also: G_i leads to increased K⁺ influx during repolarization. This shorted the plateau phase of the ventricular action potential, which means there is less time for calcium to rush in, and so there is less Ca²⁺ for contraction

M₂ receptors are G_i protien coupled. This means there is less PKA, less sodium current influx and so it takes longer to reach threshold and get a AP.

Also, G_i protiens lead to increased K⁺ in current upon repolarization, which sets the membrane potnetial even further from threshold (takes more Na⁺ influx to reach threshold, so it takes longer...)

Agonist for muscarinic receptors (M1, M2, M3)

This is an acetic acid ester, so it is susceptible to AChE.

This has a B-methyl group so it is not active at nicotinic receptors.

Quaternary amine with positive charge, poor lipid solubility, doesn't absorb well or get to CNS

Agonist for muscarinic receptors (M1, M2, M3)

This is a carbamic acid ester, so it is has negligible susceptibility to AChE.

This does not have a B-methyl group so it is active a nicotinic receptors.

Quaternary amine with positive charge, poor lipid solubility, doesn't absorb well or get to CNS

Alkaloid Agonist of Muscarinic Receptors.

Tends to be used topically.

Shows selectivity for post-synaptic M₁ receptors in sympathetic ganglia, cauing an increase in BP via the Direct Muscarinic Pathway]

Agonist of muscarinic receptors.

Alkaloid, from a mushroom poison, not used clincally.

Antagonist for Muscarinic Receptors

Atropie derivative, but acts as depressant in doses used in humans.

Readily absorbs across membranes.

Used in patch forms to treat motion sickness

Antagonist for muscarinic receptors

Atropine derivative

Used specifically to treat intestinal hyper-motility (diarrhea) through muscarinic receptors and other secret affects on smooth muscle, not yet well understood.

Anatgonist for muscarininc receptors

Atropine derivative.

Used to treat COPD/Asthma. Delivered locally by inhaler.

Charged quarternary amine, so it does nto absorb out of the respiratory system well, and does not get into the CNS. This makes for fewer side effects.

Anatgonist for muscarininc receptors

Atropine derivative.

Used to treat COPD/Asthma. Delivered locally by inhaler.

Charged quarternary amine, so it does not absorb out of the respiratory system well, and does not get into the CNS. This makes for fewer side effects.

Plus: Reduced effects at M₂ receptors (so there is no ACh release caused because previously released ACh can get to the M₂ receptor to reduce the further release)

Long half-life, so you only have to take it once-a-day

Unique! B₃ adrenergic agonist.

Used to treat urinary bladder incontinence!

Antagonist for Muscarinic Receptors

Used to treat urinary urgency.

Anatgonist for muscarininc receptors.

Used to treat urinary urgency.

Anatgonist for muscarininc receptors.

Used to treat urinary urgency.