Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
P Blier, C de Montign. Differential effect of gepirone on presynaptic and postsynaptic serotonin receptors: single-cell recording studies. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:1973935. |
the concurrent microiontophoretic application of gepirone readily blocked the effect of 5-ht on dorsal hippocampus pyramidal neurons, but not on dorsal raphe 5-ht neurons, thus indicating that gepirone is a partial agonist at postsynaptic 5-ht1a receptors and a full agonist at somatodendritic 5-ht1a receptors. |
1990-09-05 |
2023-08-11 |
rat |
P Blier, C de Montign. Differential effect of gepirone on presynaptic and postsynaptic serotonin receptors: single-cell recording studies. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:1973935. |
it is proposed that gepirone, being a partial agonist at postsynaptic 5-ht1a receptors, fails to desensitize them; whereas, because of its full agonistic activity at the somatodendritic 5-ht1a receptor, it desensitizes this autoreceptor with long-term administration. |
1990-09-05 |
2023-08-11 |
rat |
F D Yocc. Neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-HT1A receptors. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:1973941. |
neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-ht1a receptors. |
1990-09-05 |
2023-08-11 |
Not clear |
F D Yocc. Neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-HT1A receptors. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:1973941. |
preclinical neurochemical studies indicate that buspirone and gepirone bind selectively to presynaptic (dorsal raphe) and postsynaptic (hippocampus, cortex) 5-hydroxytryptamine1a (5-ht1a) receptor binding sites. |
1990-09-05 |
2023-08-11 |
Not clear |
F D Yocc. Neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-HT1A receptors. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:1973941. |
furthermore, in functional neurochemical and electrophysiologic receptor studies, azapirones in general display partial agonist activity at postsynaptic 5-ht1a receptors linked negatively to adenyl cyclase and appear to demonstrate a similar profile on hippocampal ca1 pyramidal neurons sensitive to the effects of 5-ht. |
1990-09-05 |
2023-08-11 |
Not clear |
F D Yocc. Neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-HT1A receptors. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:1973941. |
these results suggest that the efficacy seen in clinical trials of anxiety and depression may be related to buspirone's and gepirone's complex interaction with presynaptic and postsynaptic 5-ht1a receptors, which initiate long-term changes in central 5-ht neurotransmission. |
1990-09-05 |
2023-08-11 |
Not clear |
D S Robinson, K Rickels, J Feighner, L F Fabre, R E Gammans, R C Shrotriya, D R Alms, J J Andary, M E Messin. Clinical effects of the 5-HT1A partial agonists in depression: a composite analysis of buspirone in the treatment of depression. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:2198303. |
clinical effects of the 5-ht1a partial agonists in depression: a composite analysis of buspirone in the treatment of depression. |
1990-09-05 |
2023-08-11 |
Not clear |
D S Robinson, K Rickels, J Feighner, L F Fabre, R E Gammans, R C Shrotriya, D R Alms, J J Andary, M E Messin. Clinical effects of the 5-HT1A partial agonists in depression: a composite analysis of buspirone in the treatment of depression. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:2198303. |
buspirone, a serotonin (5-hydroxytryptamine, 5-ht) partial agonist active at the 5-ht1a receptor subtype, was evaluated in the treatment of depression in a series of five placebo-controlled, parallel group studies involving 382 patients with dsm-iii major depression and significant associated anxiety symptoms (both hamilton depression [ham-d] and hamilton anxiety [ham-a] scales greater than or equal to 18). |
1990-09-05 |
2023-08-11 |
Not clear |
D S Robinson, K Rickels, J Feighner, L F Fabre, R E Gammans, R C Shrotriya, D R Alms, J J Andary, M E Messin. Clinical effects of the 5-HT1A partial agonists in depression: a composite analysis of buspirone in the treatment of depression. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:2198303. |
gepirone, an analogue of buspirone with highly selective binding affinity for the 5-ht1a receptor subtype, also shows promise of antidepressant efficacy in preliminary controlled clinical trials. |
1990-09-05 |
2023-08-11 |
Not clear |
D S Robinson, K Rickels, J Feighner, L F Fabre, R E Gammans, R C Shrotriya, D R Alms, J J Andary, M E Messin. Clinical effects of the 5-HT1A partial agonists in depression: a composite analysis of buspirone in the treatment of depression. Journal of clinical psychopharmacology. vol 10. issue 3 Suppl. 1990-09-05. PMID:2198303. |
these data suggest that azapirones, which as partial agonists modulate 5-ht1a receptor function, have clinically important antidepressant properties. |
1990-09-05 |
2023-08-11 |
Not clear |
J L Rausch, S M Stahl, R L Hauge. Cortisol and growth hormone responses to the 5-HT1A agonist gepirone in depressed patients. Biological psychiatry. vol 28. issue 1. 1990-09-04. PMID:1973905. |
cortisol and growth hormone responses to the 5-ht1a agonist gepirone in depressed patients. |
1990-09-04 |
2023-08-11 |
human |
J L Rausch, S M Stahl, R L Hauge. Cortisol and growth hormone responses to the 5-HT1A agonist gepirone in depressed patients. Biological psychiatry. vol 28. issue 1. 1990-09-04. PMID:1973905. |
the 5-ht1a agonist properties of gepirone were used to test for effects on serum cortisol levels in humans, 90 min after a 10 mg oral dose. |
1990-09-04 |
2023-08-11 |
human |
P Martin, R J Beninger, M Hamon, A J Puec. Antidepressant-like action of 8-OH-DPAT, a 5-HT1A agonist, in the learned helplessness paradigm: evidence for a postsynaptic mechanism. Behavioural brain research. vol 38. issue 2. 1990-08-13. PMID:2141988. |
in animal models of depression, the 5-ht1a agonists, 8-hydroxy-2-(di-n-propylamino)tetralin (8-oh-dpat), buspirone, gepirone and ipsapirone administered i.p. |
1990-08-13 |
2023-08-11 |
rat |
G H Dreteler, W Wouters, P R Saxen. Comparison of the cardiovascular effects of the 5-HT1A receptor agonist flesinoxan with that of 8-OH-DPAT in the rat. European journal of pharmacology. vol 180. issue 2-3. 1990-08-13. PMID:2142096. |
the cardiovascular responses to flesinoxan and 8-oh-dpat in the anaesthetized wistar were inhibited by the putative 5-ht1a antagonists methiothepin, buspirone, spiroxatrine and 8-meo-c1epat (8-methoxy-2-(n-2-cholroethyl-n-n-propylamino)tetralin). |
1990-08-13 |
2023-08-11 |
rat |
P M Whitaker-Azmitia, L J Molino, J Caruso, A V Sheme. Serotonergic agents restore appropriate decision-making in neonatal rats displaying dopamine D1 receptor-mediated vacillatory behavior. European journal of pharmacology. vol 180. issue 2-3. 1990-08-13. PMID:2365008. |
behaviors measured on day 15 revealed that skf 38393-mediated behavior was effectively blocked by sch 23390 (a selective d1 antagonist), serotonin receptor agonists specific for the 5-ht1a receptor (buspirone and ipsapirone), and the serotonin uptake inhibitor clomipramine. |
1990-08-13 |
2023-08-11 |
rat |
R M Murphy, F P Zemla. Selective serotonin1A/1B agonists differentially affect spinal nociceptive reflexes. Neuropharmacology. vol 29. issue 5. 1990-07-25. PMID:2356002. |
several days after spinal transection at t10, rats were injected intraperitoneally at 20 min intervals, with increasing doses (0, 0.1, 0.4, 2.0, 9.0 mg/kg) of either a 5-ht1a selective agonist (8-oh-dpat, buspirone) or a 5-ht1b agonist (mcpp, tfmpp). |
1990-07-25 |
2023-08-11 |
rat |
R M Murphy, F P Zemla. Selective serotonin1A/1B agonists differentially affect spinal nociceptive reflexes. Neuropharmacology. vol 29. issue 5. 1990-07-25. PMID:2356002. |
the 5-ht1a agonist 8-oh-dpat and buspirone, significantly increased in a dose-dependent manner the receptive field areas of the three reflexes, with the following log ed50 values (nmol/kg): ventroflexion reflex--buspirone (2.75), 8-oh-dpat (2.70); dorsiflexion reflex--buspirone (2.91), 8-oh-dpat (2.67); lateral flexion reflex--buspirone (3.51), 8-oh-dpat (2.77). |
1990-07-25 |
2023-08-11 |
rat |
R M Murphy, F P Zemla. Selective serotonin1A/1B agonists differentially affect spinal nociceptive reflexes. Neuropharmacology. vol 29. issue 5. 1990-07-25. PMID:2356002. |
the hypersensitivity of the reflexes after pretreatment with buspirone was effectively blocked by the 5-ht1a selective antagonist spiperone, at all doses (0.001, 0.01, 0.1 and 1.0 mg/kg) tested. |
1990-07-25 |
2023-08-11 |
rat |
C W Mathes, E R Smith, B R Popa, J M Davidso. Effects of intrathecal and systemic administration of buspirone on genital reflexes and mating behavior in male rats. Pharmacology, biochemistry, and behavior. vol 36. issue 1. 1990-07-11. PMID:2349270. |
buspirone was studied to determine whether the detailed profile of male sexual behavior observed following treatment with the prototypical 5-ht1a ligand, 8-oh-dpat, can be generalized to other 5-ht1a agonist drugs. |
1990-07-11 |
2023-08-11 |
rat |
C W Mathes, E R Smith, B R Popa, J M Davidso. Effects of intrathecal and systemic administration of buspirone on genital reflexes and mating behavior in male rats. Pharmacology, biochemistry, and behavior. vol 36. issue 1. 1990-07-11. PMID:2349270. |
we conclude that buspirone affects sexual behavior very much like dpat or other 5-ht1a drugs, to the extent known. |
1990-07-11 |
2023-08-11 |
rat |