Irreversible antagonists

Phenoxybenzamine (PBZ), sold under the brand names Dibenzyline and Dibenyline, is a non-selective, irreversible alpha blocker.

Naloxazone is an irreversible μ-opioid receptor antagonist which is selective for the μ1 receptor subtype. Naloxazone produces very long lasting antagonist effects as it forms a covalent bond to the active site of the μ-opioid receptor, thus making it impossible for the molecule to unbind and blocking the receptor permanently until the receptor is recycled by endocytosis.

type of antagonist that binds permanently to a receptor, either by forming a covalent bond to the active site, or alternatively just by binding so tightly that the rate of dissociation is effectively zero at relevant time scales

right|thumb|250px|class=skin-invert-image|Metaphit as a methanesulfonate salt

JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the MOR antagonist alvimopan. In addition, it is structurally distinct from other KOR antagonists such as norbinaltorphimine. JDTic has been used to create crystal structures of KOR [ ].

chemical compound

Pindobind is a compound developed by researchers associated with Stanford University, identified as a central nervous system depressant, which generated a response in animals reducing offensive actions such as chasing, while also notably reducing tendencies of the test animal to evade when stimulated to do so. It acts as an irreversible beta blocker and irreversible 5-HT1A receptor antagonist.