Target half-life vs. species and organ/tissue
| Target | Inactivating agent | Comment | Parameter | Species | Organ/tissue | Subregion | Recovery half-life | Reference |
|---|---|---|---|---|---|---|---|---|
| Dopamine D1 receptor | EEDQ | Young (1.5 months) | Rat | Brain | Striatum | 1.4 d (34 h) | Fuxe et al. (1987) | |
| EEDQ | Young (1.5 months) | Rat | Brain | Claustrum | 1.8 d (43 h) | Fuxe et al. (1987) | ||
| EEDQ | Young (1.5 months) | Rat | Brain | Olfactory tubercle | 1.0 d (25 h) | Fuxe et al. (1987) | ||
| EEDQ | Young (1.5 months) | Rat | Brain | N. accumbens | 0.9 d (22 h) | Fuxe et al. (1987) | ||
| Alpha1-adrenoceptor | PBZ | Rat | Brain | Cortex | 5 d (120 h) | McKernan and Campbell (1982) | ||
| PBZ | Rat | Brain | Brain stem | 6 d (144 h) | McKernan and Campbell (1982) | |||
| PBZ | Rabbit | Brain | Forebrain | 10.8 d (259 h) | Hamilton and Reid (1985) | |||
| PBZ | Rabbit | Brain | Hindbrain | 13.3 d (319 h) | Hamilton and Reid (1985) | |||
| PBZ | Rabbit | Spleen | — | 3.6 d (86 h) | Hamilton et al. (1984) | |||
| PBZ | Rat | Submaxillary gland | — | 1.4 d (33 h) | Sladeczek and Bockaert (1983) | |||
| PBZ | Rat | Liver | — | 1.8 d (42 h) | Lynch et al. (1983) | |||
| Alpha2-adrenoceptor | Benextramine | Golden hamster | Kidney | — | 1.3 d (31 h) | Taouis et al. (1987) | ||
| Benextramine | Golden hamster | Adipose tissue | — | 1.9 d (46 h) | Taouis et al. (1987) | |||
| PBZ | Rabbit | Brain | Forebrain | 6.1 d (146 h) | Hamilton and Reid (1985) | |||
| PBZ | Rabbit | Brain | Hindbrain | 4.6 d (110 h) | Hamilton and Reid (1985) | |||
| PBZ | Rabbit | Spleen | — | 1.6 d (38 h) | Hamilton and Reid (1985) | |||
| EEDQ | Rat | Brain | Cortex | 4.1 d (98 h) | Adler et al. (1985) | |||
| EEDQ | Ex vivo slices | Agonist inhibition of NA release | Rat | Brain | Cortex | 2.4 d (58 h) | Adler et al. (1985) | |
| EEDQ | Ex vivo slices | Agonist inhibition of 5-HT release | Rat | Brain | Cortex | 4.6 d (110 h) | Adler et al. (1985) | |
| EEDQ | Antagonist-labeled | Rat | Brain | Cortex | 4.9 d (118 h) | Ribas et al. (1998) | ||
| EEDQ | Agonist-labeled | Rat | Brain | Cortex | 7.4 d (178 h) | Ribas et al. (1998) | ||
| EEDQ | Rat | Brain | Cortex | 3.9 d (94 h) | Barturen and Garcia-Sevilla (1992) | |||
| EEDQ | Rat | Brain | Locus coeruleus | 1.5 d (37 h) | Pineda et al. (1997) | |||
| EEDQ | NA neuronal cell firing in vivo | Rat | Brain | Locus coeruleus | 0.6 d (14 h) | Pineda et al. (1997) | ||
| EEDQ | Rat | Brain | Brain stem | 2.6 d (62 h) | Barturen and Garcia-Sevilla (1992) | |||
| EEDQ | Rat | Brain | Hippocampus | 4.3 d (103 h) | Barturen and Garcia-Sevilla (1992) | |||
| EEDQ | Rat | Brain | Hypothalamus | 2.1 d (50 h) | Barturen and Garcia-Sevilla (1992) | |||
| EEDQ | Rat | Brain | Striatum | 2.1 d (50 h) | Barturen and Garcia-Sevilla (1992) | |||
| EEDQ | Ex vivo slices | Rat | Brain | Cortex | 18.5 d (445 h) | Agneter et al. (1993) | ||
| EEDQ | Ex vivo slices | Agonist inhibition of NA release | Rat | Brain | Cortex | 0.8-2.7 d (20-64 h) | Agneter et al. (1993) | |
| EEDQ | Young (approximately 2 months) | Mouse | Brain | — | 5.3 d (126 h) | Durcan et al. (1994) | ||
| Beta2-adrenoceptor | BAAM | Guinea-pig | Lung | — | 3.8-5 d (90–120 h)* | Nelson et al. (1986) | ||
| 5-HT1A receptor | EEDQ | Mature-Aged (approximately 6–12 months) | Rat | Brain | Cortex | 7.7 d (185 h) | Keck and Lakoski (1996a) | |
| EEDQ | Rat | Brain | Cortex | 5.2 d (124 h) | Pinto and Battaglia (1994) | |||
| EEDQ | Rat | Brain | Cortex | 2.8 d (67 h) | Vinod et al. (2001) | |||
| EEDQ | Rat | Brain | Cortex layers | 3.9-4.3 d (94–103 h) | Raghupathi et al. (1996a) | |||
| EEDQ | Mature-Aged (approximately 6–12 months) | Rat | Brain | Hippocampus | 1.8 d (43 h) | Keck and Lakoski (1996b) | ||
| EEDQ | Rat | Brain | Hippocampus | 4.7 d (113 h) | Gozlan et al. (1994) | |||
| EEDQ | Rat | Brain | Hippocampus | 5.3 d (127 h) | Vinod et al. (2001) | |||
| EEDQ | Rat | Brain | Hippocampus | 2.7 d (65 h) | Bolanos et al. (1991) | |||
| EEDQ | Rat | Brain | Lateral septum | 4.0 d (96 h) | Gozlan et al. (1994) | |||
| EEDQ | Rat | Brain | Dentate gyrus | 4.2 d (101 h) | Gozlan et al. (1994) | |||
| EEDQ | Rat | Brain | Parietal cortex | 3.9 d (94 h) | Gozlan et al. (1994) | |||
| EEDQ | Rat | Brain | Hippocampal subareas | 2.3-3.6 d (55–86 h) | Raghupathi et al. (1996a) | |||
| EEDQ | Rat | Brain | Dorsal raphe | 3.2 d (77 h) | Gozlan et al. (1994) | |||
| EEDQ | Rat | Brain | Dorsal raphe | 2.7 d (69 h) | Bolanos et al. (1991) | |||
| EEDQ | Rat | Brain | Dorsal raphe | 2.8 d (67 h) | Raghupathi et al. (1996a) | |||
| 5-HT1B receptor | EEDQ | Rat | Brain | Cortex | 8.9 d (213 h) | Pinto and Battaglia (1994) | ||
| 5-HT2 receptor | EEDQ | Rat | Brain | Cortex | approximately 4.5 d (approximately 108 h) | Battaglia et al. (1986) | ||
| 5-HT2A receptor | EEDQ | Rat | Brain | Cortex | 2.9 d (70 h) | Gozlan et al. (1994) | ||
| EEDQ | Rat | Brain | Cortex | 2.5 d (58.9 h) | Pinto and Battaglia (1994) | |||
| EEDQ | Rat | Brain | Cortex | 2.6-3.3 d (62–79 h) | Raghupathi et al. (1996b) | |||
| EEDQ | Rat | Brain | Caudate-Putamen | 9.0 d (216 h) | Raghupathi et al. (1996b) | |||
| MOP | Clocinnamox | Mouse | Brain | — | 2.7-4.2 d (65–101 h) | Burke et al. (1994); Zernig et al. (1996) | ||
| Clocinnamox | Thermal heat pain in vivo | Rhesus monkey | N/A | N/A | 6.3-6.6 d (151–158 h) | Zernig et al. (1994) | ||
| DAT | RTI-76 | Rat | Brain | Striatum | 2.1-2.9 d (50–70 h) | Kimmel et al. (2000) | ||
| RTI-76 | Rat | Brain | Nucleus accumbens | 1.9-2.0 d (46–48 h) | Kimmel et al. (2000) | |||
| RTI-76 | Intrastriatal RTI-76 | Rat | Brain | Striatum | 6.3 d (151 h) | Fleckenstein et al. (1996) | ||
| DEEP-NCS | Intrastriatal DEEP-NCS | Vmax & Km change | Rat | Brain | Striatum | 6.1 d (146 h) | Rego et al. (1999) | |
| DEEP-NCS | Intrastriatal DEEP-NCS | Ex vivo DA reuptake | Rat | Brain | Striatum | 5.3 d (127 h) | Rego et al. (1999) | |
| DEEP-NCS | Intrastriatal DEEP-NCS | Receptor number | Rat | Brain | Striatum | 5.8 d (138 h) | Rego et al. (1999) | |
| SERT | RTI-76 | Rat | Brain | Hippocampus | 3.4 d (82 h) | Vicentic et al. (1999) | ||
| RTI-76 | Rat | Brain | Striatum | 3.8 d (91 h) | Vicentic et al. (1999) | |||
| MAO A | Clorgyline | Rat | Liver | — | 2.6-3.1 d (62–74 h) | Corte and Tipton (1980) | ||
| Clorgyline | Rat | Liver | — | 3.5 d (84 h) | Egashira and Kamijo (1979) | |||
| MAO B | Deprenyl | Rat | Brain | — | 7.9 d (190 h) | Felner and Waldmeier (1979) | ||
| Deprenyl | Pig | Brain | — | 6.5 d (156 h) | Oreland et al. (1990) | |||
| Deprenyl | Baboon | Brain | — | approximately 30 d (approximately 720 h) | Arnett et al. (1987) | |||
| Deprenyl | Human | Brain | Several regions, healthy & PD | approximately 40 d (approximately 960 h) | Fowler et al. (1994) | |||
| Deprenyl | Rat | Brain | Caudate | 9.2 d (221 h) | Youdim and Tipton (2002) | |||
| Rasagiline | Rat | Brain | Caudate | 9.6 d (230 h) | Youdim and Tipton (2002) | |||
| Pargyline | Rat | Brain | Caudate | 13 d (312 h) | Goridis and Neff (1971) | |||
| Pargyline | Rat | Brain | Hypothalamus | 10 d (240 h) | Goridis and Neff (1971) | |||
| Pargyline | Rat | Brain | Cerebellum | 9.1 d (218 h) | Goridis and Neff (1971) | |||
| Pargyline | Rat | Brain | — | 9.1 d (218 h) | Planz et al. (1972a) | |||
| Benmoxine | Rat | Brain | — | 10.3 d (247 h) | Planz et al. (1972a) | |||
| 3A2O | Rat | Brain | — | 10.9 d (262 h) | Planz et al. 1972a) | |||
| 3A2O | Rat | Brain homogenate | — | 10.9 d (262 h) | Planz et al. (1972b) | |||
| 3A2O | Rat | Brain mitochondria | — | 10.9 d (262 h) | Planz et al. (1972b) | |||
| Pargyline | Rat | Brain | — | 9.1 d (218 h) | Planz et al. (1972b) | |||
| Leucine incorporation | Rat | Brain | — | 9.6 d (230 h) | Planz et al. (1972b) | |||
| Nialamide | Rat | Heart | — | 10.4 d (250 h) | Planz et al. (1972b) | |||
| Nialamide | Rat | Heart | — | 12.9 d (310 h) | Planz et al. (1972b) | |||
| 3A2O | Rat | Liver homogenate | — | 4.1 d (98 h) | Planz et al. (1972b) | |||
| 3A2O | Rat | Liver mitochondria | — | 4.0 d (96 h) | Planz et al. (1972b) | |||
| Benmoxine | Rat | Liver | — | 3.9 d (94 h) | Planz et al. (1972b) | |||
| Pargyline | Rat | Liver | — | 4.3 d (103 h) | Planz et al. (1972b) | |||
| Leucine incorporation | Rat | Liver mitochondria | — | 3.7 d (89 h) | Planz et al. (1972b) | |||
| Deprenyl | Rat | Liver | — | 2.6 d (62 h) | Egashira and Kamijo (1979) | |||
| Pargyline | Rat | Liver | — | 3.5 d (84 h) | Erwin and Deitrich (1971) | |||
| Pargyline | Rat | Liver | — | 4.0 d (96 h) | Planz et al. (1972a) | |||
| Benmoxine | Rat | Liver | — | 3.9 d (94 h) | Planz et al. (1972a) | |||
| 3A2O | Rat | Liver | — | 4.1 d (98 h) | Planz et al. (1972a) | |||
| MDL72974A | Human | Platelets | — | approximately 7 d (approximately 168 h) | Hinze et al. (1990) | |||
| Pargyline | Rat | Submaxillary gland | — | 3.8 d (91 h) | Goridis and Neff (1971) | |||
| Nialamide | Rat | Submandibular gland | — | 6.0 d (144 h) | Planz et al. (1972b) | |||
| Benmoxine | Rat | Submandibular gland | 4.1 d (98 h) | Planz et al. (1972b) | ||||
| Leucine incorporation | Rat | Submandibular gland | — | 4.2 d (101 h) | Planz et al. (1972b) | |||
| Pargyline | Rat | Superior cervical ganglion | — | 4.6 d (110 h) | Goridis and Neff (1971) | |||
| 3A2O | Rat | Small intestine | Mucus layer | 4.0 d (96 h) | Planz et al. (1972a) | |||
| 3A2O | Rat | Small intestine | Muscularis layer | 0.5 d (12 h) | Planz et al. (1972a) | |||
| Deprenyl | Rat | Liver | — | 2.3 d (55 h) | Youdim and Tipton (2002) | |||
| Rasagiline | Rat | Liver | — | 2.2 d (53 h) | Youdim and Tipton (2002) | |||
| — | Turnover in dermal fibroblasts | Mouse | N/A | — | 3.3 d (79 h) | Swovick et al. (2018) | ||
| AChE | — | Leucine incorporation | Rat | Brain | Cortex | 2.8 d (67 h) | Wenthold et al. (1974) | |
| Soman | Young (approximately 1.5 months) | Rat | Brain | BLA | 5.9 d (141 h)* | Prager et al. (2014) | ||
| Soman | Young (approximately 1.5 months) | Rat | Brain | Prelimbic cortex | 7.7 d (185 h)* | Prager et al. (2014) | ||
| Soman | Young (approximately 1.5 months) | Rat | Brain | Piriform cortex | 8.0 d (193 h)* | Prager et al. (2014) | ||
| Soman | Young (approximately 1.5 months) | Rat | Brain | Hippocampus | 6.6 d (159 h)* | Prager et al. (2014) |
BAAM, bromoacetyl-alprenolol menthane; MOP, μ opioid receptor; DAT, dopamine reuptake transporter; SERT, serotonin reuptake transporter; TryH, tryptophan hydroxylase; PD, Parkinson’s disease; MAO, monoamine oxidase; 3A2O, 3-amino-2-oxazolidinone; BLA, basolateral amygdala; PBZ, phenoxybenzamine.
*Graphically estimated.