Receptors

Front 1

Striated muscle nicotinic receptor

Back 1

(a1)2 B1 d E

Front 2

Fetal muscle nicotinic receptor

Back 2

(a1)2 B1 d y

Front 3

Autonomic ganglia nicotinic receptors

Back 3

(a3)2 (B4)3

Front 4

Brain nicotinic receptors

Back 4

(a4)2 (B4)3; (a7)5; (a3)2 (B4)3

(a7)5 is highly Ca2+ permeable- others are permeable to Na/K

Front 5

M1 and M3 receptor

Back 5

Gq/11- activates PLCB- PIP2 hydrolysis- IP3 and DAG and cause SM contractions in viscera through Ca2+-CaM dependent activation of MLCK which prosphorylates MLC and htis initiates contraction

Front 6

Endothelial M3

Back 6

Increase in Ca2+-calmodulin, activates eNOS which converts arginine to No and citrulline. NO activates cGMP- relaxation of smooth muscle

Front 7

M1 in neurones

Back 7

activation inhibits a K+ conductance known as the M current. This produces a slow EPSP. The M current is mediated by Ku7 family and they are activated by PIP2 binding to their C terminus. M1 activation induced depletion of PIP2 causes inhibition

Front 8

M2 (and M4)

Back 8

Gi- found in the heart

a subunit inhibits AC- decrease cAMP and PKA, decrease phosphorylation of VGCa2+C, decrease excitability of heart m

By subunit- opens GIRK of heart and this decreases HR

Expressed presynaptically and decreases CaV activity (decrease Cav phosphorylation) at nerve endings and decrease trasmitter release

Front 9

a1

Back 9

Gq/11 coupled- PLC activation- increase in IP3, DAG and Ca2+

Dilation of pupils; vasoconstriction to vessels to viscera, brain and skin; salivary secretion; decreased GI motility and tone (relax SM), localized sweat secretion- hands; piloerection; contraction of trigone and sphincter of bladder; ejaculation of sperm; increased gluconeogenesis and glycogenolysis

Front 10

a2

Back 10

Gi

Inhibition of neurotransmitter release, platelet aggregation, vasoconstriction, inhibition of insulin release from B cells

Front 11

B1

Back 11

Gs coupled- in the heart

Increased force of myocardial contraction, increased heart rate

B1 in the kidney stimulates renin secretion

Front 12

B2

Back 12

Gs coupled

Relaxation of tracheal and bronchial SM; relaxation of SM of bvs supplying the heart and SKM; relaxation of uterine SM (non pregnant); hepatic glycogenolysis

Front 13

B3

Back 13

G2 coupled

Lipolysis, thermogenesis

Front 14

P2X1-7

Back 14

Stimulated by ATP, signal and homo/heterodimers, ligand gated ion channels

Front 15

P2X 2,4,6

Back 15

Main subtypes in postsynaptic neurones- critical for initation of AP

P2X2/3 receptors on subepithelial sensory nn are responsible for visceral pain

Front 16

P2X1

Back 16

In smooth muscle, stimulation causes contraction of the vas deferens to propel sperm into the ejaculate. Mice lacking these receptors are infertile

Front 17

P2Y

Back 17

GPCRs, some are activated by ATP but can be activated by ADP, UTP etc

Front 18

Adensine receptors- A1, A2a and A3 (P1)

Back 18

GPCRs

A1- decreases rate and force of contraction of heart- adenosine is given IV to stop supraventricular tachycardia

A1 and A2- inhibitory effects on many CNS neurons

Front 19

AT2

Back 19

Angiotensin II receptor, activation causes vasodilation by generation of NO- increase cGMP

Binding of AII in some cells can inhibit prolieration, mediate differentiation in neural tissue and can induce apoptosis

Front 20

AT4

Back 20

Angiotensin receptor, may be activated by AIV, located not just in brain, activation has been proposed as a strategy for memory enhancement esp Alzheimer's disease

Front 21

H1

Back 21

Gq/11, histamine receptor imp in inflammation.

Causes SM contraction in the ileum, bronchioles and uterus, blood vessel dilation- mediated by NO, itching via activation of pruritoceptors, triple response

Front 22

H2

Back 22

G2- histamine receptor imp in gastric acid secretion

Front 23

H3

Back 23

Gi- histamine receptor that is an imp inhibitory autoreceptor in the CNS

Front 24

H4

Back 24

Gi- decrease chemotaxis and cytokine release

Front 25

B1 and B2

Back 25

Gq coupled, B1 are upregulated in inflammation and the primary agonist is des-Arg bradykinin. B2 are constitutively expressed and are activated by bradykinin and kallidin

Activation on endothelium mediates vasodilation via PGI2 and NO

Activation also activates nociceptors

Front 26

NK1 receptor

Back 26

Neurokinin receptor- Gq coupled activated by substance P. Mast cell degranulation, SM contraction, vasodilation and neuronal sensitisation

Front 27

NK2

Back 27

Neurokinin receptor- Gq coupled activated by neurokinin A, Mast cell degranulation, SM contraction, vasodilation and neuronal sensitisation

Front 28

FMR2

Back 28

Formyl peptide receptor 2- Gi coupled. Activated by Annexin-A1 and LXA4, anti-inflammatory- decrease neutrophil chemotaxis and degranulation of mast cells

Front 29

BLT1 and BLT2

Back 29

GPCR receptor for LTB4- chemoattraction, activate neutrophils

Front 30

CysLt1

Back 30

Activated by LTD4, bronchoconstricion, increase vascular permeability and mucus secretion

Front 31

CysLT2

Back 31

activated by LTC4, bronchoconstricion,increase vascular permeability and mucus secretion

Front 32

DP1

Back 32

Gs coupled- when PGD2 binds- vasodilation, inhibit platelet aggregation, relaxes GI/uterine muscle

Front 33

EP2

Back 33

Gs coupled- when PGE2 binds= bronchodilation, vasodilation and relaxation of GI muscle

Front 34

EP4

Back 34

Gs coupled, activated by PGE2- cause sensitisation of nociceptors

Front 35

IP receptor

Back 35

Gs coupled, activated by PGI2- vasodilation and inhibition of platelet aggregation

Front 36

EP1

Back 36

Gq coupled, activated by PGE2 to cause bronchial/GI muscle contraction

Front 37

FP

Back 37

Gq coupled, activated by PGF2a- uterine contraction and bronchoconstriction (cats and dogs)

Front 38

TP

Back 38

Gq coupled, activated by PGD2 and TXA2- bronchoconstriction, vasoconstriction and platelet aggregation

Front 39

DP2

Back 39

Gi coupled

Front 40

EP3

Back 40

Gi coupled- GI muscle contraction, fever, inhibition of GA secretion and increase gastric mucous secretion

Front 41

5HT1A,B,D,F

Back 41

Gi GPCRs

Front 42

5HT2A-C

Back 42

Gq coupled

Front 43

5HT3

Back 43

ionotropic receptor

Front 44

A1

Back 44

Gi coupled, decrease rate and force of contraction in heart, bronchoconstriction, presynaptic inhibition, decrease glutamate release, induces sleep, endogenous antiepileptic

Front 45

A2

Back 45

2 types- A and B, both G2 coupled, vasodilation (including in the coronary aa) decrease activation neutrophils

Front 46

A3

Back 46

Gq/11 coupled, decrease eosinophil activation, esp in lungs