m2, org med

Protein molecule usually embedded within the cell membrane with part of its structure exposed on the outside of the cell.

Site where the drug exerts its characteristic effects or where the drug acts.

in receptor it Contain specific regions that react with

Enables physiological messages to be communicated from the drug or endogenous substances

Most drugs act by combining with ________ in the biological system

• Drug Receptor Interactions are also referred to as

a drug or endogenous substance that has an affinity for a receptor & produces a biological response

agonist + receptor =

agonist + antagonist+ receptor =

antagonist + receptor =

a drug that has affinity for a receptor but does not activate it to produce a response

are referred to as having affinity for the receptor but has no intrinsic activity

antagonist or agonist

it produces an action or response.

antagonist or agonist

is a muscle whose contraction moves a part of the body directly.

antagonist or agonist

is a substance which initiates a physiological response when combined with a receptor.

antagonist or agonist

is a drug which imitates the action of neurotransmitters in the brain.

antagonist or agonist

it produces its opposite action or response.

antagonist or agonist

is a muscle whose action counteracts that of agonist,

antagonist or agonist

is a substance which interferes with or inhibits the
physiological action of another.

antagonist or agonist

a drug that blocks neuratransmitters

Predicts that the biological response is directly related to the number of receptors occupied by the agonist

Response ceases when the drug dissociates from the receptor

antagonists occupy with high affinity but do not produce a
biological response

Predicts that the biological response is proportional to the rate of the drug-receptor complex.

Activation is proportional to the total number of encounters of a drug with its receptor.

in rate theory, the basis of a drug's activity is the
________ of the onet and offset of the drug's binding to the receptor.

Predicts that as the drug approaches the inactive state of the receptor it induces a specific conformational change that leads to effective drug binding and biological response

According to this theory, antagonists induce a nonspecific conformational change that fail to produce the
desired biological response

For this theory, it suggests that there are two types of specific receptor conformational perturbations: One leading to the biological response &the other to no activity

in this theory rate and ratio of their existence determines the observed biological response

in THE MACROMOLECULAR PERTURBATION THEORY, it is the combination of ________

Postulates that the receptor is always in the equillibrium between active and inactive states

Agonists function by shifting the equilibrium to the active state while antagonists prevent the active state

This can account for the activity of inverse agonists which can produce responses opposite to that of an agonist

what are the DIFFERENT TYPES OF MEMBRANE-BOUND RECEPTORS

Binding of a drug or any endogenous substance to its receptor allows physiological messages to be communicated from the drug into the cells without having to go through the cell membrane, This kind of method of communication is termed as ______

what type of membrane bound receptor is Receptors controlling ion channels are an integral part of the ion channel. Binding of a messenger induces a change in shape, which results in the rapid opening of the ion channel.

Receptors controlling ion channels are called _____________
receptors. They consist of five protein subunits with the receptor binding site being present on one or more of the subunits.

opened and closed by the changes in the membrane potential

what are the ions of voltage-gated ion channels ?

in voltage-gated ion channels, . Sodium channels are responsible for impulse conduction in the sensory nerve fibers

in voltage-gated ion channels, : voltage- gated ga channels & ATP sensitive K channels work together to secrete insulin from β- cells of the pancreas

in voltage-gated ion channels, Voltage- dependent calcium
channels are found in pacemaker cells & skeletal, cardiac & smooth muscles

what type of membrane bound receptor is action is regulated by binding of a ligand to the channel

in LIGAND- GATED ION CHANNELS, ligands includes _______, ________, _______, Action can be modified by drugs (e.g. BZDs)

in LIGAND- GATED ION CHANNELS, the binding of acetylcholine results in Na influx, generation of an action potential and activation of skeletal muscle contractions

in LIGAND- GATED ION CHANNELS, located in the CNS. Binding results in the influx of cl & hyperpolarization of the responsive cells

true or false

Binding of a neurotransmitter to an anion channel receptor causes a conformationat change in the protein subunits such that the second transmembrane domain of each subunit rotates to open the channel.

what type of membrane bound receptor is, A single peptide with 7 membrane -spanning regions linked to a G- protein

G-PROTEIN COUPLED RECEPTORS is also known as

true or false

in G-PROTEIN COUPLED RECEPTORS, Binding of ligand catalyzes the exchange of GDP for G-protein bound guanosine triphosphate (GTP)

in G-PROTEIN COUPLED RECEPTORS, CTP-G- Protein interacts with specific _____________ systems to elicit biological response

in G-PROTEIN COUPLED RECEPTORS, determine what Secondary Messenger in this pathway Adenylyl Cyclase

in G-PROTEIN COUPLED RECEPTORS, determine what Secondary Messenger in this pathway Phospholipase A2

in G-PROTEIN COUPLED RECEPTORS, determine what Secondary Messenger in this pathway Phospholipase C

in G-PROTEIN COUPLED RECEPTORS, in Secondary Messenger in this pathway, it is for this designated ion channels

what type of membrane bound receptor is Binding of a messenger results in the opening of a binding site for the signal protein. The latter binds and fragments, with one of the subunits departing to activate a membrane-bound enzyme.

_______ and _______ phosphorylate proteins leading to a number of effects including smooth muscle contraction, itching, systemic vasodilation and bronchoconstriction

what type of membrane bound receptor is These are receptors which are directly linked to kinase enzymes.Messenger binding results in the opening of the kinase-active site,allowing a catalytic reaction to take place

what type of membrane bound receptor has Has cystolic enzyme activity as an integral component of its structure

what type of membrane bound receptor has Binding of ligand can either activate or inhibit the cystolic enzyme activity

in TRANSMEMBRANE ENZYME - LINKED RECEPTORS, what is the most common enzyme link to a receptor

example receptor of TRANSMEMBRANE ENZYME - LINKED RECEPTORS

Not all receptors are located in the cell membrane. Some receptors are within the cell and are defined as

intracellular aka _______ or _________

The chemical messengers for intracellular receptors must be sufficiently _______ to pass through the cell membrane.

in intracellular receptors , it has 3 functional domains, in this domain it binds a medulator protein

in intracellular receptors , it has 3 functional domains, in this domain it contains the ligand binding site